标签归档：gsk

GSK232

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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。

GSK232 

GSK232 是一种高选择性的细胞渗透性 CECR2 抑制剂，具有优异的物理化学性能。

GSK232

GSK232 Chemical Structure

CAS No. : 2702984-69-6

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

GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

分子量

479.00

Formula

C21H27ClN6O3S
CAS 号

2702984-69-6
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]. Lucas SCC, et al. Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode. J Med Chem. 2020 May 28;63(10):5212-5241.

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

GSK232

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。

GSK232 

GSK232 是一种高选择性的细胞渗透性 CECR2 抑制剂，具有优异的物理化学性能。

GSK232

GSK232 Chemical Structure

CAS No. : 2702984-69-6

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

GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

分子量

479.00

Formula

C21H27ClN6O3S
CAS 号

2702984-69-6
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]. Lucas SCC, et al. Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode. J Med Chem. 2020 May 28;63(10):5212-5241.

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

GSK232

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。

GSK232 

GSK232 是一种高选择性的细胞渗透性 CECR2 抑制剂，具有优异的物理化学性能。

GSK232

GSK232 Chemical Structure

CAS No. : 2702984-69-6

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

GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

分子量

479.00

Formula

C21H27ClN6O3S
CAS 号

2702984-69-6
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]. Lucas SCC, et al. Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode. J Med Chem. 2020 May 28;63(10):5212-5241.

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

GSK121

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。

GSK121 

GSK-121 Trifluoroacetate 是选择性的 PAD4 抑制剂。

GSK121

GSK121 Chemical Structure

CAS No. : 1652591-80-4

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

GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].

分子量

501.50

Formula

C25H26F3N5O3
CAS 号

1652591-80-4
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]. Drewes G, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

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

GSK121

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。

GSK121 

GSK-121 Trifluoroacetate 是选择性的 PAD4 抑制剂。

GSK121

GSK121 Chemical Structure

CAS No. : 1652591-80-4

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

GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].

分子量

501.50

Formula

C25H26F3N5O3
CAS 号

1652591-80-4
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]. Drewes G, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

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

GSK121

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。

GSK121 

GSK-121 Trifluoroacetate 是选择性的 PAD4 抑制剂。

GSK121

GSK121 Chemical Structure

CAS No. : 1652591-80-4

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

GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].

分子量

501.50

Formula

C25H26F3N5O3
CAS 号

1652591-80-4
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]. Drewes G, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

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

GSK-3 Inhibitor XIII

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。

GSK-3 Inhibitor XIII 

GSK-3 Inhibitor XIII 是一种有效的 ATP 竞争性 GSK-3 抑制剂，Ki 为 24 nM。

GSK-3 Inhibitor XIII

GSK-3 Inhibitor XIII Chemical Structure

CAS No. : 404828-08-6

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

GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM[1][1][2].

分子量

305.38

Formula

C18H19N5
CAS 号

404828-08-6
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]. Albert C Pierce, et al. CH…O and CH…N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor. J Med Chem. 2005 Feb 24;48(4):1278-81.

    [2]. Eduardo Cruz Moraes, et al. Kinase inhibitor profile for human nek1, nek6, and nek7 and analysis of the structural basis for inhibitor specificity. Molecules. 2015 Jan 13;20(1):1176-91.

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

GSK-3 Inhibitor XIII

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。

GSK-3 Inhibitor XIII 

GSK-3 Inhibitor XIII 是一种有效的 ATP 竞争性 GSK-3 抑制剂，Ki 为 24 nM。

GSK-3 Inhibitor XIII

GSK-3 Inhibitor XIII Chemical Structure

CAS No. : 404828-08-6

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

GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM[1][1][2].

分子量

305.38

Formula

C18H19N5
CAS 号

404828-08-6
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]. Albert C Pierce, et al. CH…O and CH…N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor. J Med Chem. 2005 Feb 24;48(4):1278-81.

    [2]. Eduardo Cruz Moraes, et al. Kinase inhibitor profile for human nek1, nek6, and nek7 and analysis of the structural basis for inhibitor specificity. Molecules. 2015 Jan 13;20(1):1176-91.

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

GSK-3 Inhibitor XIII

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。

GSK-3 Inhibitor XIII 

GSK-3 Inhibitor XIII 是一种有效的 ATP 竞争性 GSK-3 抑制剂，Ki 为 24 nM。

GSK-3 Inhibitor XIII

GSK-3 Inhibitor XIII Chemical Structure

CAS No. : 404828-08-6

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

GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM[1][1][2].

分子量

305.38

Formula

C18H19N5
CAS 号

404828-08-6
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]. Albert C Pierce, et al. CH…O and CH…N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor. J Med Chem. 2005 Feb 24;48(4):1278-81.

    [2]. Eduardo Cruz Moraes, et al. Kinase inhibitor profile for human nek1, nek6, and nek7 and analysis of the structural basis for inhibitor specificity. Molecules. 2015 Jan 13;20(1):1176-91.

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

GSK199

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。

GSK199 

GSK199 是一种可逆的选择性 PAD4 抑制剂，在缺少钙离子的情况下，其 IC50 为 200 nM。

GSK199

GSK199 Chemical Structure

CAS No. : 1549811-53-1

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

GSK199 is a reversible and selective PAD4 inhibitor with an IC50 of 200 nM in the absence of calcium[1].

分子量

468.98

Formula

C24H29ClN6O2
CAS 号

1549811-53-1
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]. Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

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

Uprosertib hydrochloride(Synonyms: GSK2141795 (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。

Uprosertib hydrochloride (Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride (GSK2141795 hydrochloride) 是一种有效的，选择性的 Akt 广谱抑制剂，抑制 Akt1/Akt2/Akt3 的活性，IC50 值分别为 180/328/38 nM。

Uprosertib hydrochloride(Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride Chemical Structure

CAS No. : 1047635-80-2

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

* Please select Quantity before adding items.

Uprosertib hydrochloride 的其他形式现货产品:

Uprosertib

生物活性

Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

IC50 & Target[1]

Akt1

180 nM (IC50)

Akt2

328 nM (IC50)

Akt3

38 nM (IC50)

CDK7

2100 nM (IC50)

ROCK1

1570 nM (IC50)

ROCK2

1850 nM (IC50)

体外研究
(In Vitro)

Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

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

分子量

465.71

Formula

C18H17Cl3F2N4O2
CAS 号

1047635-80-2
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]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
Kinase Assay
[1]

For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

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

  • [1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.

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

Uprosertib hydrochloride(Synonyms: GSK2141795 (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。

Uprosertib hydrochloride (Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride (GSK2141795 hydrochloride) 是一种有效的，选择性的 Akt 广谱抑制剂，抑制 Akt1/Akt2/Akt3 的活性，IC50 值分别为 180/328/38 nM。

Uprosertib hydrochloride(Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride Chemical Structure

CAS No. : 1047635-80-2

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

* Please select Quantity before adding items.

Uprosertib hydrochloride 的其他形式现货产品:

Uprosertib

生物活性

Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

IC50 & Target[1]

Akt1

180 nM (IC50)

Akt2

328 nM (IC50)

Akt3

38 nM (IC50)

CDK7

2100 nM (IC50)

ROCK1

1570 nM (IC50)

ROCK2

1850 nM (IC50)

体外研究
(In Vitro)

Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

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

分子量

465.71

Formula

C18H17Cl3F2N4O2
CAS 号

1047635-80-2
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]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
Kinase Assay
[1]

For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

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

  • [1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.

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

Uprosertib hydrochloride(Synonyms: GSK2141795 (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。

Uprosertib hydrochloride (Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride (GSK2141795 hydrochloride) 是一种有效的，选择性的 Akt 广谱抑制剂，抑制 Akt1/Akt2/Akt3 的活性，IC50 值分别为 180/328/38 nM。

Uprosertib hydrochloride(Synonyms: GSK2141795 (hydrochloride))

Uprosertib hydrochloride Chemical Structure

CAS No. : 1047635-80-2

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

* Please select Quantity before adding items.

Uprosertib hydrochloride 的其他形式现货产品:

Uprosertib

生物活性

Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

IC50 & Target[1]

Akt1

180 nM (IC50)

Akt2

328 nM (IC50)

Akt3

38 nM (IC50)

CDK7

2100 nM (IC50)

ROCK1

1570 nM (IC50)

ROCK2

1850 nM (IC50)

体外研究
(In Vitro)

Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[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.
Clinical Trial

分子量

465.71

Formula

C18H17Cl3F2N4O2
CAS 号

1047635-80-2
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]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
Kinase Assay
[1]

For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

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]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.

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GSK-J1 lithium salt

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GSK-J1 lithium salt 

GSK-J1 lithium salt 是一种有效的 H3K27me3/me2-demethylases JMJD3/KDM6B 和 UTX/KDM6A 的抑制剂，对 KDM6B 的 IC50 值为 60 nM。

GSK-J1 lithium salt

GSK-J1 lithium salt Chemical Structure

规格 价格 是否有货
10 mg ￥700 询问价格 & 货期
25 mg ￥1150 询问价格 & 货期
50 mg ￥2050 询问价格 & 货期
100 mg ￥3400 询问价格 & 货期

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GSK-J1 lithium salt 的其他形式现货产品:

GSK-J1 GSK-J2 GSK-J4

生物活性

GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.

IC50 & Target

IC50: 60 nM (KDM6B)[2]
体外研究
(In Vitro)

GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner[1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively[3].

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

395.38

Formula

C22H22LiN5O2
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]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.

    [2]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2

    [3]. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46.
Kinase Assay
[1]

Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.

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]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.

    [2]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2

    [3]. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46.

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GSK2850163 hydrochloride

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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。

GSK2850163 hydrochloride 

GSK2850163 hydrochloride 是一个新型的肌醇需要酶-1α (IRE1α) 抑制剂，它可抑制 IRE1α 的激酶活性和 RNA 酶活性，其 IC50 值分别为 20 和 200 nM。

GSK2850163 hydrochloride

GSK2850163 hydrochloride Chemical Structure

CAS No. : 2319838-09-8

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250 mg   询价  
500 mg   询价  

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GSK2850163 hydrochloride 的其他形式现货产品:

GSK2850163

生物活性

GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

IC50 & Target

IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1]
体外研究
(In Vitro)

GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α can be reduced in a dose-dependent manner by GSK2850163 hydrochloride. Increasing concentrations of GSK2850163 hydrochloride are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163 hydrochloride: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=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

482.87

Formula

C24H30Cl3N3O
CAS 号

2319838-09-8
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]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.
Kinase Assay
[1]

In the ADP-Glo assay, GSK2850163 hydrochloride’s potency toward pIRE1α kinase activity is measured as its inhibition of an intrinsic, slowing ATP hydrolysis activity. One hundred nanoliters of dimethylsulfoxide solution of GSK2850163 hydrochloride at various concentrations is added into a 384-well plate. The reaction is carried out with 5 nM pIRE1α and 60 mM ATP in 10 mL of 50 mM Hepes buffer, pH 7.5, containing 30 mM NaCl, 10 mM MgCl2, 1 mM DTT, 0.02% Chaps, and 0.01 mg/mL bovine serum albumin. The reaction is stopped after 2 hours by adding 5 mL of ADP-Glo reagent I, which also depletes the remaining ATP. Following 1-hour incubation, 5 mL of ADP-Glo reagent II is added into the reaction, which converts the ADP product into ATP to serve as the substrate for the coupled luciferin/luciferase reaction. After 30 minutes, the plate is read on a microplate imager[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]

PANC-1 cells are seeded into six-well plates at a density of 5.0×103 cells/well in RPMI 1640 media containing 10% FBS. Cells are cotransfected with a pGL3-5x unfolded protein response element (UPRE)-luciferase reporter containing five repetitions of the XBP-1 DNA binding site and pRL-SV40 using the FuGENE6 transfection reagent. Forty-eight hours later, cells are treated with 2.5 mg/mL tunicamycin for 1 hour, followed by GSK2850163 hydrochloride treatment for 16 hours. Luciferase expression is measured using Dual-Glo Luciferase Assay kit and normalized to Renilla expression levels[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]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.

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GSK3186899(Synonyms: DDD-853651)

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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。

GSK3186899 (Synonyms: DDD-853651)

GSK3186899 (DDD-853651) 是 CRK12 的一个抑制剂，其对 L. donovani 的 EC50 值为 1.4 μM。

GSK3186899(Synonyms: DDD-853651)

GSK3186899 Chemical Structure

CAS No. : 1972617-87-0

规格 是否有货
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250 mg   询价  
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生物活性

GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.

IC50 & Target

CRK12[1].
体外研究
(In Vitro)

GSK3186899 (Compound 7) is active against L. donovani in an intra-macrophage assay with an EC50 value of 1.4 μM, and shows good selectivity against mammalian THP-1 host cells (EC50 value>50 μM). This is not as potent as reported data for amphotericin B (EC50 value of 0.07 μM in the intra-macrophage assay), but is comparable to the clinically used drugs miltefosine and paromomycin (EC50 values of 0.9 μM and 6.6 μM, respectively). GSK3186899 is also active in cidal axenic amastigote assay (EC50 value of 0.1 μM). At a concentration of 0.2 μM, GSK3186899 is cytocidal at 96 h; increasing the concentration to 1.8 μM reduced this time to 48 h. GSK3186899 demonstrates a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is also more active in a panel of Leishmania lines using human peripheral blood mononuclear cells as the host cells[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.
体内研究
(In Vivo)

In the mouse model of infection, GSK3186899 demonstrates comparable activity to the front-line drug miltefosine, reducing parasite levels by 99% when dosed orally twice a day for 10 days at 25 mg/kg. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). The non-clinical safety data for GSK3186899 suggests a suitable therapeutic window for progression into regulatory preclinical studies. Non-GLP preclinical assessment of cardiovascular effects and genotoxicity does not reveal any issues that would prevent further development. In addition, there are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested. Both the in vivo efficacy and safety profile of GSK3186899 support progression to definitive safety studies[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.
Clinical Trial

分子量

491.53

Formula

C19H28F3N7O3S
CAS 号

1972617-87-0
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]. Wyllie S, et al. Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis. Nature. 2018 Aug;560(7717):192-197.

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GSK2110183 analog 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。

GSK2110183 analog 1 

GSK2110183 analog 1 是 GSK2110183 的结构类似物。

GSK2110183 analog 1

GSK2110183 analog 1 Chemical Structure

CAS No. : 1047634-63-8

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

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GSK2110183 analog 1 的其他形式现货产品:

GSK2110183 analog 1 hydrochloride

生物活性

GSK2110183 analog 1 is the structural analogue of GSK2110183.

分子量

445.31

Formula

C18H16Cl2F2N4OS
CAS 号

1047634-63-8
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.
Animal Administration

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.

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GSK2194069

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。

GSK2194069  纯度: 99.67%

GSK2194069是有效和特异的β-酮酰还原酶（KR）抑制剂，在检测释放CoA 实验中的IC50分别为7.7±4.1nM。

GSK2194069

GSK2194069 Chemical Structure

CAS No. : 1332331-08-4

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 ￥1273 In-stock
2 mg ￥850 In-stock
5 mg ￥1350 In-stock
10 mg ￥2350 In-stock
50 mg ￥9400 In-stock
100 mg ￥15500 In-stock
200 mg   询价  
500 mg   询价  

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GSK2194069 相关产品

•相关化合物库:

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生物活性

GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA. IC50 value: Target: hFAS inhibitor

分子量

428.48

Formula

C25H24N4O3
CAS 号

1332331-08-4
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 : ≥ 100 mg/mL (233.38 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 2.3338 mL 11.6692 mL 23.3383 mL
5 mM 0.4668 mL 2.3338 mL 4.6677 mL
10 mM 0.2334 mL 1.1669 mL 2.3338 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 (5.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.83 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 (5.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.83 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 (5.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.83 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]. Hardwicke MA, et al. A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol. 2014 Sep;10(9):774-9.

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Trametinib(Synonyms: 曲美替尼; GSK1120212; JTP-74057)

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。

Trametinib (Synonyms: 曲美替尼; GSK1120212; JTP-74057) 纯度: 99.92%

Trametinib (GSK1120212; JTP-74057) 是口服有效的 MEK 抑制剂，抑制 MEK1 和 MEK2 的 IC50 分别为 2 nM。Trametinib 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。

Trametinib(Synonyms: 曲美替尼; GSK1120212; JTP-74057)

Trametinib Chemical Structure

CAS No. : 871700-17-3

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥385 In-stock
10 mg ￥350 In-stock
50 mg ￥780 In-stock
100 mg ￥1250 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].

IC50 & Target[1]

MEK1

2 nM (IC50)

MEK2

2 nM (IC50)

体外研究
(In Vitro)

Trametinib (GSK1120212;JTP-74057) (0.1-100 nM) blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). Trametinib (JTP-74057) inhibits the growth of 9 out of 10 human colorectal cancer cell lines, and they shows cell-cycle arrest at the G1 phase after drug tratment[1].
The combination of GSK2118436 and Trametinib (GSK1120212) effectively inhibits cell growth, decreases ERK phosphorylation, decreases cyclin D1 protein, and increases p27(kip1) protein in the resistant clones[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)

Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486[1].
Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model[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.
Clinical Trial

分子量

615.39

Formula

C26H23FIN5O4
CAS 号

871700-17-3
中文名称

曲美替尼
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 : 25 mg/mL (40.62 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 1.6250 mL 8.1249 mL 16.2499 mL
5 mM 0.3250 mL 1.6250 mL 3.2500 mL
10 mM 0.1625 mL 0.8125 mL 1.6250 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%HPMC  1%Tween80

    Solubility: 6.67 mg/mL (10.84 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 (4.06 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.06 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.06 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]. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with HWA486. Inflamm Res, 2012, 61(5), 445-454.

    [2]. Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol, 2011, 39(1), 23-31.

    [3]. Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett. 2011 Feb 28;2(4):320-4.

    [4]. Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369.

    [5]. Lai J, et al. Elimination of melanoma by sortase A-generated TCR-like antibody-drug conjugates (TL-ADCs) targeting intracellular melanoma antigen MART-1. Biomaterials. 2018 Sep;178:158-169.
Kinase Assay
[2]

The nonphosphorylated myelin basic protein (MBP) is coated onto an ELISA plate, and the active form of B-Raf/c-Raf is mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 µM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of Trametinib (JTP-74057). The phosphorylation of MBP is detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases are tested at 10 µM ATP[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.
Cell Assay
[2]

Cells are treated with various concentrations of Trametinib (JTP-74057) in 100 mm dishes for 3 or 4 days. Both floating and adherent cells are collected and fixed with 70% ethanol. After washing with PBS, the cells are suspended in 100 µL/mL RNase and 25 µL/mL Propidium iodide (PI) and incubated at 37°C for 30 min in the dark. The DNA content of each single cell is determined using the flow cytometer Cytomics FC500 or Guava EasyCyte plus[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 Administration
[2]

Mice[2]
Female BALB/c-nu/nu mice are used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) are inoculated subcutaneously into the right flank of the mice at 5×106 cells/100 µL/site or 1×106 cells/100 µL/site, respectively. The acetic acid-solvated form of Trametinib (JTP-74057, 0.3 mg/kg, 1 mg/kg) is dissolved in 10% Cremophor EL-10% PEG400 and is administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm3. The tumor length [L(mm)] and width [W(mm)] are measured using a microgauge twice a week after commencement of dosing, and the tumor volume is calculated using the following formula: tumor volume (mm3)=L×W×W/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.
参考文献

  • [1]. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with HWA486. Inflamm Res, 2012, 61(5), 445-454.

    [2]. Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol, 2011, 39(1), 23-31.

    [3]. Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett. 2011 Feb 28;2(4):320-4.

    [4]. Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369.

    [5]. Lai J, et al. Elimination of melanoma by sortase A-generated TCR-like antibody-drug conjugates (TL-ADCs) targeting intracellular melanoma antigen MART-1. Biomaterials. 2018 Sep;178:158-169.

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

GSK-3685032

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。

GSK-3685032  纯度: 98.53%

GSK-3685032 是一种非时间依赖、非共价、可逆的 DNMT1 选择性抑制剂，IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。

GSK-3685032

GSK-3685032 Chemical Structure

CAS No. : 2170137-61-6

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
25 mg ￥11000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GSK-3685032 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1].

IC50 & Target

DNMT1[1]
体外研究
(In Vitro)

GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM[1].
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course[1].
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription[1].
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression[1].
GSK3685032 induces DNA hypomethylation and gene activation[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[1]

Cell Line: 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells.
Concentration: 0.01-100 μM
Incubation Time: 6 days
Result: Showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM.

Cell Proliferation Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.1-1000 nM
Incubation Time: 1-6 days
Result: Exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course.

RT-PCR[1]

Cell Line: MV4-11 cells
Concentration: 10-10000 nM
Incubation Time: 4 days
Result: Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells.

Western Blot Analysis[1]

Cell Line: GDM-1 cells
Concentration: 3.2-10,000 nM
Incubation Time: 2 days
Result: Inhibited DNMT1 protein expression

体内研究
(In Vivo)

GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models[1].

Summary of mouse pharmacokinetic parameters for GSK-3685032[1]

Dose,Route Cmax
(ng/mL)		 AUC0-8hr
(h*ng/mL)		 DNAUC
(h*kg*ng/mL/mg)		 Clearance
(mL/min/kg)		 Volumedss
(L/kg)		 T1/2
(h)
2 mg/kg,IV 5103 2418 1209 13 1.3 1.8
2 mg/kg,SC 252 921 461 NA NA 2.8
2 mg/kg,SC 5473 15400 513 NA NA ND

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: MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)[1]
Dosage: 1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration: Subcutaneous injection, twice daily for 4 weeks
Result: Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.

分子量

420.53

Formula

C22H24N6OS
CAS 号

2170137-61-6
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 : 25 mg/mL (59.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3780 mL 11.8898 mL 23.7795 mL
5 mM 0.4756 mL 2.3780 mL 4.7559 mL
10 mM 0.2378 mL 1.1890 mL 2.3780 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 (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 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 (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 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 (5.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.94 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]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.

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