KDM5-C70

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

KDM5-C70 是 KDM5-C49 的细胞渗透性衍生物，是有效、选择性和细胞渗透性 KDM5 抑制剂，对 KDM5A、B 和 C 的 IC50 分别为 0.3、0.3 和 0.58 uM。

KDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively; significantly increases global levels of H3K4me3, while having little impact on H3K4me2/me1, or modifications regulated by other histone lysine demethylases, such as H3K27me3 (substrate for the KDM6 family) and H3K9me3/H3K36me3 (substrates for the KDM4 family).

KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM).KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells)treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression.Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations. Cell Viability Assay Cell Line:MM.1S myeloma cells Concentration:10-9-10-5 M Incubation Time:7 days Result:Showed antiproliferative effects after 7 days of treatment at elevated concentrations.Western Blot Analysis Cell Line:MM.1S myeloma cells Concentration:50 μM Incubation Time:7 days Result:Decreased the level of phosphorylation of retinoblastoma protein (Rb).

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KDM5 inhibitor C70

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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1596348-32-1

336.43

C17H28N4O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (297.24 mM)

O=C(OCC)C1=CC=NC(CNCC(N(CCN(C)C)CC)=O)=C1

Ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate

(-20℃)

With Ice Pack

≥ 2 years