CPUY074020

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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。

CPUY074020 

CPUY074020 是一种高效、有口服活性的组蛋白甲基转移酶 G9a 抑制剂，其 IC50 值为 2.18 μM。CPUY074020 具有抗增殖活性。

CPUY074020

CPUY074020 Chemical Structure

CAS No. : 902279-44-1

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生物活性

CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity[1].

IC50 & Target

IC50: 2.18 μM (G9a)[1]
体外研究
(In Vitro)

CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis[1].
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation[1].

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

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2 μM, 4 μM, 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cells apoptosis.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 hours
Result: Dose-dependently de-regulated H3K9 trimethylation.

体内研究
(In Vivo)

CPUY074020 exhibits reasonable PK properties, with an oral bioavailability of 55.5% and a T1/2 value of 4.0 hours at an oral dose of 10 mg/kg[1].

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

Animal Model: Mice
Dosage: 10 mg/kg
Administration: Oral administration
Result: t1/2=4.0 hours

分子量

416.52

Formula

C25H28N4O2
CAS 号

902279-44-1
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]. Chen WL, et al. Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular. Bioorg Med Chem. 2016 Nov 15;24(22):6102-6108.

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