CPUY074020

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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

CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis.CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation.Apoptosis Analysis 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 Cell Line: MCF-7 cells Concentration:2.5 μM, 5 μM, 10 μM Incubation Time:48 hours Result:Dose-dependently de-regulated H3K9 trimethylation.

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

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Others

Other Targets

Histone Methyltransferase

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902279-44-1

416.52

C25H28N4O2

>98% (HPLC)

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N(CCN1CCCC1)C2=C3C=4C(C(=C2)N5CCCCC5)=NOC4C=6C(C3=O)=CC=CC6

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(-20℃)

With Ice Pack

≥ 2 years