化合物GSK503 T1775

Product Introduction
Bioactivity


英文名: GSK503

描述: GSK503是一种高效特异性EZH2甲基转移酶抑制剂，Ki 值为3到27 nM，具有潜在的抗肿瘤活性。

激酶实验: In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively.

体外活性: GSK503能够以相近的效力抑制WT和突变型EZH2的甲基转移酶活性。在七种DLBCL细胞系的研究中，GSK503显示出对细胞生长的抑制作用，并且这种效果在与ABT737或Obatoclax联用时得到增强。[1]

体内活性: In C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. [1] In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (176.6 mM)
Ethanol : 25 mg/mL (47.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: GSK503 | Inhibitor | inhibit | GSK-503 | GSK 503 | Histone Methyltransferase

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相关库: Anti-Aging Compound Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | Target-Focused Phenotypic Screening Library | Methylation Compound Library | Reprogramming Compound Library | NO PAINS Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library

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