标签归档：shp

SHP2 protein degrader-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 protein degrader-1 

SHP2 protein degrader-1 是一种有效的 SHP2 变构抑制剂。SHP2 蛋白降解剂-1 诱导 SHP2 降解和细胞凋亡。SHP2 蛋白降解剂-1 具有研究 SHP2 相关疾病的潜力。

SHP2 protein degrader-1

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]
体外研究
(In Vitro)

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

Formula

C42H51Cl2N11O8
CAS 号

2624181-69-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2 protein degrader-1

发表于由
回复

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 protein degrader-1 

SHP2 protein degrader-1 是一种有效的 SHP2 变构抑制剂。SHP2 蛋白降解剂-1 诱导 SHP2 降解和细胞凋亡。SHP2 蛋白降解剂-1 具有研究 SHP2 相关疾病的潜力。

SHP2 protein degrader-1

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]
体外研究
(In Vitro)

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

Formula

C42H51Cl2N11O8
CAS 号

2624181-69-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2 protein degrader-1

发表于由
回复

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 protein degrader-1 

SHP2 protein degrader-1 是一种有效的 SHP2 变构抑制剂。SHP2 蛋白降解剂-1 诱导 SHP2 降解和细胞凋亡。SHP2 蛋白降解剂-1 具有研究 SHP2 相关疾病的潜力。

SHP2 protein degrader-1

SHP2 protein degrader-1 Chemical Structure

CAS No. : 2624181-69-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases[1].

IC50 & Target

SHP2[1]
体外研究
(In Vitro)

SHP2 protein degrader-1 (compound SP4) (0-200 μM; 24 hours) inhibits the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which are about 100 times higher than the activity of SHP099 (SHP2 inhibitor)[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces 54.01% apoptotic death compared with 0.13% of the control at 100 nM[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) induces cell cycle arrested at the G1 phase in Hela cells[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) significantly inhibits the phosphorylation of JNK, Erk and p38[1].
SHP2 protein degrader-1 (compound SP4) (0-200 μM; 96 hours) inhibits RAS/MAPK signaling and cellular responses by a mechanism involving inhibition of SHP2 catalytic activity[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hela cells
Concentration: 0-200  μM
Incubation Time: 24 hours
Result: Strongly inhibited the growth of Hela cells, with IC50 of 5.77 and 4.30 nM, respectively, which were about 100 times higher than the activity of SHP099 (SHP2 inhibitor).

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced 54.01% apoptotic death compared with 0.13% of the control at 100 nM. While SHP099 at 1000 nM could induce 33.74% apoptotic death compared with 0.13% of the control.

Cell Cycle Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Induced cell cycle arrested at the G1 phase in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 0-100  μM
Incubation Time: 96 hours
Result: Significantly inhibited the phosphorylation of JNK, Erk and p38.

分子量

908.83

Formula

C42H51Cl2N11O8
CAS 号

2624181-69-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zheng M, et al. Novel PROTACs for degradation of SHP2 protein. Bioorg Chem. 2021;110:104788.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2 inhibitor LY6(Synonyms: LY6)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 inhibitor LY6 (Synonyms: LY6)

SHP2 inhibitor LY6 (LY6) 是一种有效和选择性的 SHP2 抑制剂，IC50 值为 9.8 µM。SHP2 inhibitor LY6 可以抑制 SHP2 介导的细胞信号传导和增殖。

SHP2 inhibitor LY6(Synonyms: LY6)

SHP2 inhibitor LY6 Chemical Structure

CAS No. : 2296718-09-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 inhibitor LY6 (LY6) is potent and selective inhibitor of SHP2, with an IC50 of 9.8 µM. SHP2 inhibitor LY6 can inhibits SHP2-mediated cell signaling and proliferation[1].

IC50 & Target

IC50: 9.8 µM (SHP2)[1]
分子量

564.46

Formula

C30H27Cl2N3O4
CAS 号

2296718-09-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wu X, et, al. Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2. J Med Chem. 2019 Feb 14;62(3):1125-1137.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2 inhibitor LY6(Synonyms: LY6)

发表于由
回复

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 inhibitor LY6 (Synonyms: LY6)

SHP2 inhibitor LY6 (LY6) 是一种有效和选择性的 SHP2 抑制剂，IC50 值为 9.8 µM。SHP2 inhibitor LY6 可以抑制 SHP2 介导的细胞信号传导和增殖。

SHP2 inhibitor LY6(Synonyms: LY6)

SHP2 inhibitor LY6 Chemical Structure

CAS No. : 2296718-09-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 inhibitor LY6 (LY6) is potent and selective inhibitor of SHP2, with an IC50 of 9.8 µM. SHP2 inhibitor LY6 can inhibits SHP2-mediated cell signaling and proliferation[1].

IC50 & Target

IC50: 9.8 µM (SHP2)[1]
分子量

564.46

Formula

C30H27Cl2N3O4
CAS 号

2296718-09-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wu X, et, al. Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2. J Med Chem. 2019 Feb 14;62(3):1125-1137.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2 inhibitor LY6(Synonyms: LY6)

发表于由
回复

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2 inhibitor LY6 (Synonyms: LY6)

SHP2 inhibitor LY6 (LY6) 是一种有效和选择性的 SHP2 抑制剂，IC50 值为 9.8 µM。SHP2 inhibitor LY6 可以抑制 SHP2 介导的细胞信号传导和增殖。

SHP2 inhibitor LY6(Synonyms: LY6)

SHP2 inhibitor LY6 Chemical Structure

CAS No. : 2296718-09-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2 inhibitor LY6 (LY6) is potent and selective inhibitor of SHP2, with an IC50 of 9.8 µM. SHP2 inhibitor LY6 can inhibits SHP2-mediated cell signaling and proliferation[1].

IC50 & Target

IC50: 9.8 µM (SHP2)[1]
分子量

564.46

Formula

C30H27Cl2N3O4
CAS 号

2296718-09-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wu X, et, al. Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2. J Med Chem. 2019 Feb 14;62(3):1125-1137.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP504

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP504 

SHP504 是 SHP2 磷酸酶的抑制剂，其对SHP21–525 的IC50 值为21 μM。

SHP504

SHP504 Chemical Structure

CAS No. : 2222280-83-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP504 is a SHP2 phosphatase inhibitor, with an IC50 of 21 μM for SHP21–525[1].

分子量

446.84

Formula

C23H15ClN4O4
CAS 号

2222280-83-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Michelle Fodor, et al. Dual Allosteric Inhibition of SHP2 Phosphatase. ACS Chem Biol. 2018 Mar 16;13(3):647-656.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-9 

SHP2-IN-9是一种特异性的 SHP2 抑制剂 (IC50 =1.174 μM)，具有增强的血脑屏障渗透性。SHP2-IN-9 对 SHP2 的选择性是 SHP1 的 85 倍。SHP2-IN-9 在体内抑制 SHP2 介导的细胞信号转导和癌细胞增殖，并抑制宫颈癌肿瘤和胶质母细胞瘤的生长。

SHP2-IN-9

SHP2-IN-9 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo[1].

体外研究
(In Vitro)

SHP2-IN-9 (compound 2) could effectively inhibit SHP2-mediated cell signaling pathways in cancer (cervix cancer, human pancreatic cancer, large cell lung cancer and mouse glioma cell) by inhibiting the phosphorylation of Paxillin, affecting the regulation of the PI3K/AKT pathway and cell proliferation by causing the cell cycle arrest and inducing the early apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

385.46

Formula

C20H20FN3O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ma Y, et al. Structure-based discovery of a specific SHP2 inhibitor with enhanced blood-brain barrier penetration from PubChem database. Bioorg Chem. 2022;121:105648.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-9 

SHP2-IN-9是一种特异性的 SHP2 抑制剂 (IC50 =1.174 μM)，具有增强的血脑屏障渗透性。SHP2-IN-9 对 SHP2 的选择性是 SHP1 的 85 倍。SHP2-IN-9 在体内抑制 SHP2 介导的细胞信号转导和癌细胞增殖，并抑制宫颈癌肿瘤和胶质母细胞瘤的生长。

SHP2-IN-9

SHP2-IN-9 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo[1].

体外研究
(In Vitro)

SHP2-IN-9 (compound 2) could effectively inhibit SHP2-mediated cell signaling pathways in cancer (cervix cancer, human pancreatic cancer, large cell lung cancer and mouse glioma cell) by inhibiting the phosphorylation of Paxillin, affecting the regulation of the PI3K/AKT pathway and cell proliferation by causing the cell cycle arrest and inducing the early apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

385.46

Formula

C20H20FN3O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ma Y, et al. Structure-based discovery of a specific SHP2 inhibitor with enhanced blood-brain barrier penetration from PubChem database. Bioorg Chem. 2022;121:105648.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-9 

SHP2-IN-9是一种特异性的 SHP2 抑制剂 (IC50 =1.174 μM)，具有增强的血脑屏障渗透性。SHP2-IN-9 对 SHP2 的选择性是 SHP1 的 85 倍。SHP2-IN-9 在体内抑制 SHP2 介导的细胞信号转导和癌细胞增殖，并抑制宫颈癌肿瘤和胶质母细胞瘤的生长。

SHP2-IN-9

SHP2-IN-9 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo[1].

体外研究
(In Vitro)

SHP2-IN-9 (compound 2) could effectively inhibit SHP2-mediated cell signaling pathways in cancer (cervix cancer, human pancreatic cancer, large cell lung cancer and mouse glioma cell) by inhibiting the phosphorylation of Paxillin, affecting the regulation of the PI3K/AKT pathway and cell proliferation by causing the cell cycle arrest and inducing the early apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

385.46

Formula

C20H20FN3O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ma Y, et al. Structure-based discovery of a specific SHP2 inhibitor with enhanced blood-brain barrier penetration from PubChem database. Bioorg Chem. 2022;121:105648.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-8 

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

SHP2-IN-8

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.

分子量

398.35

Formula

C17H21Cl2N5S
CAS 号

1801692-60-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tang K, Zhao M, Wu YH, et al. Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors. Eur J Med Chem. 2022;230:114106.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PHPS1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PHPS1 

PHPS1 是一种有效的选择性 Shp2 抑制剂，对 Shp2，Shp2-R362K，Shp1，PTP1B 和 PTP1B-Q 的 Ki 值分别为 0.73，5.8，10.7，5.8 和 0.47 μM。

PHPS1

PHPS1 Chemical Structure

CAS No. : 314291-83-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].

IC50 & Target

Ki: 0.73 μM (Shp2), 5.8 μM (Shp2-R362K), 10.7 μM (Shp1), 5.8 μM (PTP1B), 0.47 μM (PTP1B-Q)[1]
体外研究
(In Vitro)

PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells[1].
PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human cancer cell lines MDA-MB-435, HCT-116 (colon carcinoma), HCT-15 (colon carcinoma), PC-3 (prostate carcinoma) HT-29 (colon carcinoma), NCI-H661 (lung carcinoma), and Caki-1 (kidney carcinoma)
Concentration: 30 μM
Incubation Time: 6 days
Result: Resulted in a reduction in cell number of between 0% (Caki-1) to 74% (HT-29).

Western Blot Analysis[1]

Cell Line: Madin-Darby canine kidney (MDCK) cells
Concentration: 5, 10, 20 μM
Incubation Time: 5, 15, 60, 120, 360 minutes
Result: Inhibited HGF/SF (1 unit/mL)-induced phosphorylation and thus activation of Erk1/2 over a time period of 15 min to 6 h. In contrast, transient phosphorylation of Erk1/2 after 5 min was not affected.
Exhibited no effect on HGF/SF-induced activation of PI3K/Akt or Stat3.

体内研究
(In Vivo)

PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr-/- mice less susceptible to atherosclerosis development[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ldlr-/- (005061) mice[2]
Dosage: 3 mg/kg
Administration: Intraperitoneal (i.p.) injection; every day during the last week on the high-fat diet.
Result: Revealed a significant decrease in atherosclerotic plaque size in the aorta compared with the other two groups.

分子量

465.44

Formula

C21H15N5O6S
CAS 号

314291-83-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Klaus Hellmuth, et al. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-Throughput Docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80.

    [2]. Jia Chen, et al. SHP2 Inhibitor PHPS1 Protects Against Atherosclerosis by Inhibiting Smooth Muscle Cell Proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP099

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP099  纯度: 99.66%

SHP099是有效，选择性，有口服活性的 SHP2 抑制剂，IC50 值为70 nM。

SHP099

SHP099 Chemical Structure

CAS No. : 1801747-42-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥620 In-stock
5 mg ￥800 In-stock
10 mg ￥1450 In-stock
50 mg ￥4800 In-stock
100 mg ￥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SHP099 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Phosphatase Inhibitor Library

生物活性

SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM[1].

IC50 & Target

IC50: 70 nM (SHP2)[1]
体外研究
(In Vitro)

The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells[1]. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

After a single doses of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

352.26

Formula

C16H19Cl2N5
CAS 号

1801747-42-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12 mg/mL (34.07 mM; Need ultrasonic)

H2O : 1 mg/mL (2.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8388 mL 14.1941 mL 28.3881 mL
5 mM 0.5678 mL 2.8388 mL 5.6776 mL
10 mM 0.2839 mL 1.4194 mL 2.8388 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (28.39 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.2 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.2 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.2 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.2 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.2 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.2 mg/mL (3.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 12.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 5.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution

  • 6.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.67 mg/mL (1.90 mM); Clear solution

  • 7.

    请依序添加每种溶剂： 1% DMSO    99% saline

    Solubility: ≥ 0.13 mg/mL (0.37 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

    [2]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.
Kinase Assay
[1]

The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

    [2]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP099 hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP099 hydrochloride  纯度: 99.87%

SHP099 hydrochloride是有效，选择性，有口服活性的 SHP2 抑制剂，IC50值为70 nM。

SHP099 hydrochloride

SHP099 hydrochloride Chemical Structure

CAS No. : 2200214-93-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥684 In-stock
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
50 mg ￥2880 In-stock
100 mg ￥5280 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SHP099 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Phosphatase Inhibitor Library

生物活性

SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM[1].

IC50 & Target

IC50: 70 nM (SHP2)[1]
体外研究
(In Vitro)

The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells[1]. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

After a single doses of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

388.72

Formula

C16H20Cl3N5
CAS 号

2200214-93-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 4.1 mg/mL (10.55 mM; Need ultrasonic and warming)

H2O : ≥ 2.5 mg/mL (6.43 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5725 mL 12.8627 mL 25.7255 mL
5 mM 0.5145 mL 2.5725 mL 5.1451 mL
10 mM 0.2573 mL 1.2863 mL 2.5725 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 50% PEG300    50% saline

    Solubility: 20 mg/mL (51.45 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.43 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

    [2]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

    [3]. Carmine Fedele, et al. SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models. bioRxiv. April 25, 2018.
Kinase Assay
[1]

The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

    [2]. Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

    [3]. Carmine Fedele, et al. SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models. bioRxiv. April 25, 2018.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

RMC-4630(Synonyms: SHP2-IN-7)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RMC-4630 (Synonyms: SHP2-IN-7) 纯度: 99.19%

RMC-4630 (SHP2-IN-7) 是 一种 SHP2 抑制剂，来自专利 WO2018013597。

RMC-4630(Synonyms: SHP2-IN-7)

RMC-4630 Chemical Structure

CAS No. : 2172652-48-9

规格 价格 是否有货 数量
5 mg ￥4500 In-stock
10 mg ￥8000 In-stock
25 mg ￥16500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

RMC-4630 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Phosphatase Inhibitor Library

生物活性

RMC-4630 (SHP2-IN-7) is an SHP2 inhibitor extracted from patent WO2018013597[1].

IC50 & Target

SHP2[1]
分子量

450.99

Formula

C20H27ClN6O2S
CAS 号

2172652-48-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (110.87 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2173 mL 11.0867 mL 22.1734 mL
5 mM 0.4435 mL 2.2173 mL 4.4347 mL
10 mM 0.2217 mL 1.1087 mL 2.2173 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. WO2018013597

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

三点位加热磁力搅拌器SHP-200-MP 搅拌罐/搅拌器

发表于由

【简单介绍】

三点位加热磁力搅拌器SHP-200-MP,三工位搅拌热板；230伏交流电，50赫兹
三个独立的搅拌或加热/搅拌位置，但尺寸仅为23-5/8英寸长x 10-5/8英寸宽(60 x 27厘米)
用于强磁耦合和搅拌能力的强力磁铁
在每个位置轻松容纳一个2升烧杯
铝/硅合金顶板提供均匀的板温
闪烁的“热”警告灯指示温度高于50℃

【详细说明】

三点位加热磁力搅拌器SHP-200-MP

产品描述：

三个独立控制的位置单元只需要一个电源。同时运行三个单独的测试，或在相同条件下运行多个样本。

请注意:自2022年6月起，型号为SB162-3的Stuart搅拌热板现已更名为Cole-Parmer，型号为SHP-200-MP。所有相同的伟大功能和规格，只是有一个新的和改进的外观。

主要特点：

三个独立的搅拌或加热/搅拌位置，但尺寸仅为23-5/8英寸长x 10-5/8英寸宽(60 x 27厘米)

用于强磁耦合和搅拌能力的强力磁铁

在每个位置轻松容纳一个2升烧杯

铝/硅合金顶板提供均匀的板温

闪烁的“热”警告灯指示温度高于50℃

技术参数

面板材质 铝硅合金
搅拌位置数 3
顶板长度 16CM
顶板宽度 16CM
加热功率, W 3 x 700
温度范围 50-325℃
最大负载能力 2kg
搅拌速度范围, rpm 0 – 1500
外形尺寸(宽x d x h), mm 600 x 270 x 110
插头类型 欧洲和英国标准
净重, kg 11
电源 230V, 50Hz, 2250W

三点位加热磁力搅拌器SHP-200-MP

三工位搅拌热板；230伏交流电，50赫兹

SHP2-D26

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-D26 

SHP2-D26 是首个高效的 SHP2 降解剂。SHP2-D26 诱导 SHP2 降解时需要与 VHL-1 和 SHP2 蛋白结合，并且是类泛素化修饰依赖和蛋白酶体依赖的。

SHP2-D26

SHP2-D26 Chemical Structure

CAS No. : 2458219-65-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent[1].

IC50 & Target

SHP2[1]
体外研究
(In Vitro)

SHP2-D26 (0, 3, 10, 30, 100, 300 nM; 12 hours) effectively reduces SHP2 protein in a dosedependent manner, with DC50 values of 6.0 nM, 2.6 nM in KYSE520 and MV-4-11 cells, respectively[1].
SHP2-D26 (100 nM; 0, 2, 4, 8, 12, 24 hours) reduces the SHP2 protein level within 4 h and completes SHP2 depletion with 8 h in KYSE520 and MV-4-11 cells[1].
SHP2-D26 (0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells; 4 days) achieves IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells
Incubation Time: 4 days
Result: Achieved IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 0, 3, 10, 30, 100, 300 nM
Incubation Time: 12 hours
Result: Reduced SHP2 protein in a dosedependent manner, with DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: KYSE520 and MV-4-11 cells
Concentration: 100 nM
Incubation Time: 0, 2, 4, 8, 12, 24 hours
Result: Reduced the SHP2 protein level within 4 h and completed SHP2 depletion with 8 h.

分子量

1115.89

Formula

C56H79ClN12O6S2
CAS 号

2458219-65-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein [published correction appears in J Med Chem. 2021 Jan 14;64(1):906-908]. J Med Chem. 2020;63(14):7510-7528.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SHP2-IN-6 hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SHP2-IN-6 hydrochloride  纯度: 98.74%

SHP2-IN-6 hydrochloride 是一种有效的 SHP2 抑制剂，IC50 值为 25.8 nM，详细信息请参见专利 WO2017211303A1，compound 7。

SHP2-IN-6 hydrochloride

SHP2-IN-6 hydrochloride Chemical Structure

CAS No. : 2169223-49-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5420 In-stock
5 mg ￥4800 In-stock
10 mg ￥8000 In-stock
25 mg ￥16500 In-stock
50 mg ￥26000 In-stock
100 mg ￥40000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SHP2-IN-6 hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Phosphatase Inhibitor Library

生物活性

SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor with an IC50 of 25.8 nM. SHP2-IN-6 hydrochloride is extracted from patent WO2017211303A1, compound 7[1].

体外研究
(In Vitro)

SHP2-IN-6 inhibits the proliferation of KYSE-520 cells with an IC50 of 2.17 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

513.00

Formula

C22H27ClF2N6O2S
CAS 号

2169223-49-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 115 mg/mL (224.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9493 mL 9.7466 mL 19.4932 mL
5 mM 0.3899 mL 1.9493 mL 3.8986 mL
10 mM 0.1949 mL 0.9747 mL 1.9493 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5.75 mg/mL (11.21 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (11.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5.75 mg/mL (11.21 mM); Clear solution

    此方案可获得 ≥ 5.75 mg/mL (11.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cunbo Ma, et al. Novel heterocyclic derivatives useful as shp2 inhibitors. WO2017211303A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务