CPI-455

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

一种有效的、特异性组蛋白去甲基化酶泛 KDM5 抑制剂，对 KDM5A、KDM5B 和 KDM5C 的生化 IC50 分别为 10、3 和 14 nM。

A potent, specific histone demethylase pan-KDM5 inhibitor with biochemical IC50 of 10, 3 and 14 nM for KDM5A, KDM5B and KDM5C, respectively; shows substantially weaker potency toward KDM4C and KDM7B (200- and 770-fold, respectively) and no inhibition of KDM2B, KDM3B or KDM6A; dose-dependently increases in H3K4 methylation in multiple cell lines, decreases the number of drug-tolerant persister cancer cells (DTPs) in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

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Animal Model:Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.) Dosage:50 mg/kg or 70 mg/kg (combined with anti–B7-H4).Administration:IP, daily, 14-28 days.Result:Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge.Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

CPI455 | CPI 455

Chromatin/Epigenetic

Histone Demethylase

KDM5A

Cancer

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1628208-23-0

278.3086

C16H14N4O

>98% (HPLC)

DMSO: ≥ 34 mg/mL

N#CC1=C(NC(C2=CC=CC=C2)=C(C(C)C)C3=O)N3N=C1

Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-

(-20℃)

With Ice Pack

≥ 2 years