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CHR-6494 TFA

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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。

CHR-6494 TFA 

CHR-6494 TFA 是一种有效的选择性 haspin 抑制剂，IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。

CHR-6494 TFA

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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

* Please select Quantity before adding items.

CHR-6494 TFA 的其他形式现货产品:

CHR-6494

生物活性

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[3].

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

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.

分子量

406.36

Formula

C18H17F3N6O2
CAS 号

1458630-17-5
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]. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18.

    [2]. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943.

    [3]. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.

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

CHR-6494 TFA

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。

CHR-6494 TFA 

CHR-6494 TFA 是一种有效的选择性 haspin 抑制剂，IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。

CHR-6494 TFA

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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

* Please select Quantity before adding items.

CHR-6494 TFA 的其他形式现货产品:

CHR-6494

生物活性

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[3].

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

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.

分子量

406.36

Formula

C18H17F3N6O2
CAS 号

1458630-17-5
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]. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18.

    [2]. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943.

    [3]. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.

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

CHR-6494 TFA

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。

CHR-6494 TFA 

CHR-6494 TFA 是一种有效的选择性 haspin 抑制剂，IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。

CHR-6494 TFA

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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

* Please select Quantity before adding items.

CHR-6494 TFA 的其他形式现货产品:

CHR-6494

生物活性

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[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.
体内研究
(In Vivo)

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[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.

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.

分子量

406.36

Formula

C18H17F3N6O2
CAS 号

1458630-17-5
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]. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18.

    [2]. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943.

    [3]. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.

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

Allo-aca TFA

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。

Allo-aca TFA 

Allo-aca TFA 是一种瘦素肽模拟物，是一种有效的、特异性的瘦素受体 (leptin receptor) 拮抗剂肽。Allo-aca TFA在多种体外和体内模型中阻断瘦素信号传导和作用。

Allo-aca TFA

Allo-aca TFA 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.

Allo-aca TFA 的其他形式现货产品:

Allo-aca

生物活性

Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models[1][2].

体外研究
(In Vitro)

Allo-aca TFA inhibits leptin-induced proliferation of MDA-MB-231 cells at 50 pM concentration. Allo-aca TFA inhibits leptin-induced proliferation of MCF-7 cells with an IC50 of 200 pM[1].
Allo-aca TFA at 250 nmol/L reduces VEGF-dependent leptin mRNA expression in both cell lines below base levels. Allo-aca TFA inhibits VEGF mitogenic effects. Allo-aca TFA inhibits VEGF-induced chemotaxis and chemokinesis in RF/6A retinal endothelial cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In an MDA-MB-231 orthotopic mouse xenograft model, Allo-aca TFA administered subcutaneously significantly extends the average survival time from 15.4 days (untreated controls) to 24 and 28.1 days at 0.1 and 1mg/kg/day doses, respectively[1].

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

1188.21

Formula

C50H76F3N13O17
Sequence Shortening

{H-allo}-TE-{Nva}-VALSR-{Aca}-NH2
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]. Otvos L Jr, et al. Efficacy of a leptin receptor antagonist peptide in a mouse model of triple-negative breast cancer. Eur J Cancer. 2011;47(10):1578-1584.

    [2]. Coroniti R, et al. Designer Leptin Receptor Antagonist Allo-aca Inhibits VEGF Effects in Ophthalmic Neoangiogenesis Models [published correction appears in Front Mol Biosci. 2016 Nov 18;3:75]. Front Mol Biosci. 2016;3:67. Published 2016 Oct 13.

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

Allo-aca TFA

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。

Allo-aca TFA 

Allo-aca TFA 是一种瘦素肽模拟物，是一种有效的、特异性的瘦素受体 (leptin receptor) 拮抗剂肽。Allo-aca TFA在多种体外和体内模型中阻断瘦素信号传导和作用。

Allo-aca TFA

Allo-aca TFA 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.

Allo-aca TFA 的其他形式现货产品:

Allo-aca

生物活性

Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models[1][2].

体外研究
(In Vitro)

Allo-aca TFA inhibits leptin-induced proliferation of MDA-MB-231 cells at 50 pM concentration. Allo-aca TFA inhibits leptin-induced proliferation of MCF-7 cells with an IC50 of 200 pM[1].
Allo-aca TFA at 250 nmol/L reduces VEGF-dependent leptin mRNA expression in both cell lines below base levels. Allo-aca TFA inhibits VEGF mitogenic effects. Allo-aca TFA inhibits VEGF-induced chemotaxis and chemokinesis in RF/6A retinal endothelial cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In an MDA-MB-231 orthotopic mouse xenograft model, Allo-aca TFA administered subcutaneously significantly extends the average survival time from 15.4 days (untreated controls) to 24 and 28.1 days at 0.1 and 1mg/kg/day doses, respectively[1].

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

1188.21

Formula

C50H76F3N13O17
Sequence Shortening

{H-allo}-TE-{Nva}-VALSR-{Aca}-NH2
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]. Otvos L Jr, et al. Efficacy of a leptin receptor antagonist peptide in a mouse model of triple-negative breast cancer. Eur J Cancer. 2011;47(10):1578-1584.

    [2]. Coroniti R, et al. Designer Leptin Receptor Antagonist Allo-aca Inhibits VEGF Effects in Ophthalmic Neoangiogenesis Models [published correction appears in Front Mol Biosci. 2016 Nov 18;3:75]. Front Mol Biosci. 2016;3:67. Published 2016 Oct 13.

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

Allo-aca TFA

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。

Allo-aca TFA 

Allo-aca TFA 是一种瘦素肽模拟物，是一种有效的、特异性的瘦素受体 (leptin receptor) 拮抗剂肽。Allo-aca TFA在多种体外和体内模型中阻断瘦素信号传导和作用。

Allo-aca TFA

Allo-aca TFA 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.

Allo-aca TFA 的其他形式现货产品:

Allo-aca

生物活性

Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models[1][2].

体外研究
(In Vitro)

Allo-aca TFA inhibits leptin-induced proliferation of MDA-MB-231 cells at 50 pM concentration. Allo-aca TFA inhibits leptin-induced proliferation of MCF-7 cells with an IC50 of 200 pM[1].
Allo-aca TFA at 250 nmol/L reduces VEGF-dependent leptin mRNA expression in both cell lines below base levels. Allo-aca TFA inhibits VEGF mitogenic effects. Allo-aca TFA inhibits VEGF-induced chemotaxis and chemokinesis in RF/6A retinal endothelial 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)

In an MDA-MB-231 orthotopic mouse xenograft model, Allo-aca TFA administered subcutaneously significantly extends the average survival time from 15.4 days (untreated controls) to 24 and 28.1 days at 0.1 and 1mg/kg/day doses, 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.
分子量

1188.21

Formula

C50H76F3N13O17
Sequence Shortening

{H-allo}-TE-{Nva}-VALSR-{Aca}-NH2
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]. Otvos L Jr, et al. Efficacy of a leptin receptor antagonist peptide in a mouse model of triple-negative breast cancer. Eur J Cancer. 2011;47(10):1578-1584.

    [2]. Coroniti R, et al. Designer Leptin Receptor Antagonist Allo-aca Inhibits VEGF Effects in Ophthalmic Neoangiogenesis Models [published correction appears in Front Mol Biosci. 2016 Nov 18;3:75]. Front Mol Biosci. 2016;3:67. Published 2016 Oct 13.

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

CL2E-SN38 TFA

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。

CL2E-SN38 TFA 

CL2E-SN-38 TFA 是一种结构稳定的抗体-SN-38 偶联物，是抗体药物偶联物 (ADC) 的一部分。SN-38 是喜树碱中 Irinotecan 的活性代谢物，是一种拓扑异构酶 I 抑制剂。

CL2E-SN38 TFA

CL2E-SN38 TFA 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

CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor[1].

分子量

1845.96

Formula

C88H119F3N14O26
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]. Lianqi Liu, et al. Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.

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CL2E-SN38 TFA

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。

CL2E-SN38 TFA 

CL2E-SN-38 TFA 是一种结构稳定的抗体-SN-38 偶联物，是抗体药物偶联物 (ADC) 的一部分。SN-38 是喜树碱中 Irinotecan 的活性代谢物，是一种拓扑异构酶 I 抑制剂。

CL2E-SN38 TFA

CL2E-SN38 TFA Chemical Structure

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

CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor[1].

分子量

1845.96

Formula

C88H119F3N14O26
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]. Lianqi Liu, et al. Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.

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

CL2E-SN38 TFA

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。

CL2E-SN38 TFA 

CL2E-SN-38 TFA 是一种结构稳定的抗体-SN-38 偶联物，是抗体药物偶联物 (ADC) 的一部分。SN-38 是喜树碱中 Irinotecan 的活性代谢物，是一种拓扑异构酶 I 抑制剂。

CL2E-SN38 TFA

CL2E-SN38 TFA 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

CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor[1].

分子量

1845.96

Formula

C88H119F3N14O26
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]. Lianqi Liu, et al. Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.

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

CREB-IN-1 TFA

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。

CREB-IN-1 TFA 

CREB-IN-1 TFA 是一种有效的，具有口服活性的 CREB 抑制剂 (IC50=0.18 µM)。CREB-IN-1 TFA 能够抑制乳腺癌细胞的生长。

CREB-IN-1 TFA

CREB-IN-1 TFA 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

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth[1].

IC50 & Target

IC50: 0.18 µM (CREB)[1]
体外研究
(In Vitro)

CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 µM; 24 hours) inhibits CREB-mediated gene transcription with an IC50 of 0.18 µM[1].
CREB-IN-1 TFA (100 µM; 3 days) shows potent activities in MDA-MB-231 (GI50=0.38 µM) and MDA-MB-468 (GI50=0.021 µM) cells[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: HEK 293T cells
Concentration: 100 µM
Incubation Time: 24 hours
Result: Inhibited CREB-mediated gene transcription with an IC50 of 0.18 µM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 100 µM
Incubation Time: 3 days
Result: Showed potent activities in MDA-MB-231 (GI50 =0.38 µM) and MDA-MB-468 (GI50 =0.021 µM) cells.

体内研究
(In Vivo)

CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%[1].
Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice [1].

route dose(mg/kg) t1/2(h) Tmax(h) Cmax(ng/mL) AUC0-t(ng·hr/mL) AUC0-∞((ng·hr/mL) bioavailability (F%)
IP 10 4.2 1.0 156 892 910 144
PO 20 5.5 2.00 73 468 479 38


Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO[1].

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

Animal Model: Female C57BL/6 mice[1]
Dosage: 5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H2O at 40 mg/mL and further dilutions were made using ddI H2O)
Administration: Showed much improve oral bioavailability at 38%.
Result: Showed much improve oral bioavailability at 38%.

分子量

778.06

Formula

C35H32ClF3N3O10P
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]. Peng J, et al. Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription. ACS Med Chem Lett. 2022; 13(3):388-395.

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

CREB-IN-1 TFA

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。

CREB-IN-1 TFA 

CREB-IN-1 TFA 是一种有效的，具有口服活性的 CREB 抑制剂 (IC50=0.18 µM)。CREB-IN-1 TFA 能够抑制乳腺癌细胞的生长。

CREB-IN-1 TFA

CREB-IN-1 TFA 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

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth[1].

IC50 & Target

IC50: 0.18 µM (CREB)[1]
体外研究
(In Vitro)

CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 µM; 24 hours) inhibits CREB-mediated gene transcription with an IC50 of 0.18 µM[1].
CREB-IN-1 TFA (100 µM; 3 days) shows potent activities in MDA-MB-231 (GI50=0.38 µM) and MDA-MB-468 (GI50=0.021 µM) cells[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: HEK 293T cells
Concentration: 100 µM
Incubation Time: 24 hours
Result: Inhibited CREB-mediated gene transcription with an IC50 of 0.18 µM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 100 µM
Incubation Time: 3 days
Result: Showed potent activities in MDA-MB-231 (GI50 =0.38 µM) and MDA-MB-468 (GI50 =0.021 µM) cells.

体内研究
(In Vivo)

CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%[1].
Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice [1].

route dose(mg/kg) t1/2(h) Tmax(h) Cmax(ng/mL) AUC0-t(ng·hr/mL) AUC0-∞((ng·hr/mL) bioavailability (F%)
IP 10 4.2 1.0 156 892 910 144
PO 20 5.5 2.00 73 468 479 38


Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO[1].

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

Animal Model: Female C57BL/6 mice[1]
Dosage: 5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H2O at 40 mg/mL and further dilutions were made using ddI H2O)
Administration: Showed much improve oral bioavailability at 38%.
Result: Showed much improve oral bioavailability at 38%.

分子量

778.06

Formula

C35H32ClF3N3O10P
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]. Peng J, et al. Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription. ACS Med Chem Lett. 2022; 13(3):388-395.

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

CREB-IN-1 TFA

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。

CREB-IN-1 TFA 

CREB-IN-1 TFA 是一种有效的，具有口服活性的 CREB 抑制剂 (IC50=0.18 µM)。CREB-IN-1 TFA 能够抑制乳腺癌细胞的生长。

CREB-IN-1 TFA

CREB-IN-1 TFA 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

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth[1].

IC50 & Target

IC50: 0.18 µM (CREB)[1]
体外研究
(In Vitro)

CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 µM; 24 hours) inhibits CREB-mediated gene transcription with an IC50 of 0.18 µM[1].
CREB-IN-1 TFA (100 µM; 3 days) shows potent activities in MDA-MB-231 (GI50=0.38 µM) and MDA-MB-468 (GI50=0.021 µM) 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.

Cell Viability Assay[1]

Cell Line: HEK 293T cells
Concentration: 100 µM
Incubation Time: 24 hours
Result: Inhibited CREB-mediated gene transcription with an IC50 of 0.18 µM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 100 µM
Incubation Time: 3 days
Result: Showed potent activities in MDA-MB-231 (GI50 =0.38 µM) and MDA-MB-468 (GI50 =0.021 µM) cells.

体内研究
(In Vivo)

CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%[1].
Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice [1].

route dose(mg/kg) t1/2(h) Tmax(h) Cmax(ng/mL) AUC0-t(ng·hr/mL) AUC0-∞((ng·hr/mL) bioavailability (F%)
IP 10 4.2 1.0 156 892 910 144
PO 20 5.5 2.00 73 468 479 38


Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO[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.

Animal Model: Female C57BL/6 mice[1]
Dosage: 5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H2O at 40 mg/mL and further dilutions were made using ddI H2O)
Administration: Showed much improve oral bioavailability at 38%.
Result: Showed much improve oral bioavailability at 38%.

分子量

778.06

Formula

C35H32ClF3N3O10P
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]. Peng J, et al. Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription. ACS Med Chem Lett. 2022; 13(3):388-395.

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

Goralatide TFA

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。

Goralatide TFA 

Goralatide TFA 是细胞周期进程的抑制剂。Goralatide TFA 增强了热清除人祖细胞的选择性。Goralatide TFA 具有白血病研究的潜力。

Goralatide TFA

Goralatide TFA Chemical Structure

CAS No. : 1796568-94-9

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

* Please select Quantity before adding items.

Goralatide TFA 的其他形式现货产品:

Goralatide acetate

生物活性

Goralatide TFA is an inhibitor of cell cycle progression. Goralatide TFA enhances selectivity of hyperthermic purging of human progenitor cells. Goralatide TFA has the potential for the research of leukemia[1].

分子量

601.53

Formula

C22H34F3N5O11
CAS 号

1796568-94-9
Sequence Shortening

Ac-SDKP
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]. Wierenga PK, et al. Enhanced selectivity of hyperthermic purging of human progenitor cells using Goralatide, an inhibitor of cell cycle progression. Bone Marrow Transplant. 1998;21(1):73-78.

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

GO-203 TFA

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。

GO-203 TFA  纯度: 98.00%

GO-203 TFA 是一种有效的 MUC1-C 癌蛋白抑制剂。 GO-203 TFA 是一种靶向细胞内蛋白的抗癌肽。

GO-203 TFA

GO-203 TFA Chemical Structure

CAS No. : 1222186-26-6

规格 价格 是否有货 数量
1 mg ￥900 In-stock
5 mg ￥2400 In-stock
10 mg ￥3800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GO-203 TFA 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an anti-cancer peptide for targeting intracellular proteins[1].

分子量

2426.77

Formula

C89H171F3N52O21S2
CAS 号

1222186-26-6
Sequence Shortening

RRRRRRRRRCQCRRKN
运输条件

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

  • [1]. Masanori Hasegawa, et al. Intracellular Targeting of the Oncogenic MUC1-C Protein with a Novel GO-203 Nanoparticle Formulation. Clin Cancer Res. 2015 May 15;21(10):2338-47.

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

GO-203 TFA

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。

GO-203 TFA  纯度: 98.00%

GO-203 TFA 是一种有效的 MUC1-C 癌蛋白抑制剂。 GO-203 TFA 是一种靶向细胞内蛋白的抗癌肽。

GO-203 TFA

GO-203 TFA Chemical Structure

CAS No. : 1222186-26-6

规格 价格 是否有货 数量
1 mg ￥900 In-stock
5 mg ￥2400 In-stock
10 mg ￥3800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GO-203 TFA 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an anti-cancer peptide for targeting intracellular proteins[1].

分子量

2426.77

Formula

C89H171F3N52O21S2
CAS 号

1222186-26-6
Sequence Shortening

RRRRRRRRRCQCRRKN
运输条件

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

  • [1]. Masanori Hasegawa, et al. Intracellular Targeting of the Oncogenic MUC1-C Protein with a Novel GO-203 Nanoparticle Formulation. Clin Cancer Res. 2015 May 15;21(10):2338-47.

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

GO-203 TFA

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。

GO-203 TFA  纯度: 98.00%

GO-203 TFA 是一种有效的 MUC1-C 癌蛋白抑制剂。 GO-203 TFA 是一种靶向细胞内蛋白的抗癌肽。

GO-203 TFA

GO-203 TFA Chemical Structure

CAS No. : 1222186-26-6

规格 价格 是否有货 数量
1 mg ￥900 In-stock
5 mg ￥2400 In-stock
10 mg ￥3800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GO-203 TFA 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an anti-cancer peptide for targeting intracellular proteins[1].

分子量

2426.77

Formula

C89H171F3N52O21S2
CAS 号

1222186-26-6
Sequence Shortening

RRRRRRRRRCQCRRKN
运输条件

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

  • [1]. Masanori Hasegawa, et al. Intracellular Targeting of the Oncogenic MUC1-C Protein with a Novel GO-203 Nanoparticle Formulation. Clin Cancer Res. 2015 May 15;21(10):2338-47.

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

UNC0379 TFA

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。

UNC0379 TFA 

UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂，IC50 值为 7.3 μM，对其他 15 种甲基转移酶有很好的选择性。

UNC0379 TFA

UNC0379 TFA Chemical Structure

CAS No. : 1620401-83-3

规格 价格 是否有货 数量
2 mg ￥650 In-stock
5 mg ￥1000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases[1].

IC50 & Target

SETD8/KMT5A[1]
分子量

527.58

Formula

C25H36F3N5O4
CAS 号

1620401-83-3
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: 

H2O : 100 mg/mL (189.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8954 mL 9.4772 mL 18.9545 mL
5 mM 0.3791 mL 1.8954 mL 3.7909 mL
10 mM 0.1895 mL 0.9477 mL 1.8954 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。
参考文献

  • [1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

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

UNC0379 TFA

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。

UNC0379 TFA 

UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂，IC50 值为 7.3 μM，对其他 15 种甲基转移酶有很好的选择性。

UNC0379 TFA

UNC0379 TFA Chemical Structure

CAS No. : 1620401-83-3

规格 价格 是否有货 数量
2 mg ￥650 In-stock
5 mg ￥1000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases[1].

IC50 & Target

SETD8/KMT5A[1]
分子量

527.58

Formula

C25H36F3N5O4
CAS 号

1620401-83-3
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: 

H2O : 100 mg/mL (189.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8954 mL 9.4772 mL 18.9545 mL
5 mM 0.3791 mL 1.8954 mL 3.7909 mL
10 mM 0.1895 mL 0.9477 mL 1.8954 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。
参考文献

  • [1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

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

UNC0379 TFA

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。

UNC0379 TFA 

UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂，IC50 值为 7.3 μM，对其他 15 种甲基转移酶有很好的选择性。

UNC0379 TFA

UNC0379 TFA Chemical Structure

CAS No. : 1620401-83-3

规格 价格 是否有货 数量
2 mg ￥650 In-stock
5 mg ￥1000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases[1].

IC50 & Target

SETD8/KMT5A[1]
分子量

527.58

Formula

C25H36F3N5O4
CAS 号

1620401-83-3
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: 

H2O : 100 mg/mL (189.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8954 mL 9.4772 mL 18.9545 mL
5 mM 0.3791 mL 1.8954 mL 3.7909 mL
10 mM 0.1895 mL 0.9477 mL 1.8954 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。
参考文献

  • [1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

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

Lys-CoA TFA

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。

Lys-CoA TFA 

Lys-CoA TFA 是一种选择性 p300 组蛋白乙酰转移酶 (HAT) 抑制剂 (IC50=50-500 nM)。Lys-CoA TFA 对 p300 的选择性是 PCAF 的 100 多倍 (IC50=200 μM)。Lys-CoA TFA 抑制 p300-HAT 活性依赖的转录激活。

Lys-CoA TFA

Lys-CoA TFA 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

Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation[1][2].

IC50 & Target[1]

p300

50-500 nM (IC50)

体外研究
(In Vitro)

Lys-CoA TFA (0.1 and 1 mM; 60 hours) induces a senescent phenotype in human normal melanocytes[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.

Cell Proliferation Assay[3]

Cell Line: Normal human melanocytes
Concentration: 0.1 and 1 mM
Incubation Time: 60 hours
Result: Almost completely abolished proliferation, induced high levels of SA-β-Gal, and inhibited cyclin E expression in a dose-dependent manner.

分子量

1108.82

Formula

C33H54F3N10O21P3S
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]. Cebrat M, et al. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg Med Chem. 2003;11(15):3307-3313.

    [2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000;5(3):589-595.

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