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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-iJMJD6
iJMJD6

Chemical Structure : iJMJD6

CAS No.: 899548-78-8

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iJMJD6 (inhibitor of JMJD6)

货号: PC-49244Not For Human Use, Lab Use Only.

iJMJD6 is a potent, specific small-molecule JMJD6 inhibitor that specifically binds to JMJD6 (ITC Kd=3.83 uM) and competes with α-KG and the substrate for binding, inhibits the demethylase activity of JMJD6 with IC50 of 149.6 nM.

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10 mg ￥1580 In stock
25 mg ￥2680 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

iJMJD6 is a potent, specific small-molecule JMJD6 inhibitor that specifically binds to JMJD6 (ITC Kd=3.83 uM) and competes with α-KG and the substrate for binding, inhibits the demethylase activity of JMJD6 with IC50 of 149.6 nM.
iJMJD6 suppresses the malignant phenotypes of HeLa cervical cancer cells, inhibits cell proliferation with EC50 of 1.49, 9.37, and 9.53 uM for HeLa, SMCC7721, and MCF7 cells, respectively.
iJMJD6 inhibits JMJD6-mediated demethylation in HeLa cells,inhibits the expression of oncogenes, including c-Myc, N-myc, and CCND1, inhibit the transcription of these oncogenes through inhibiting JMJD6-mediated demethylation of H4R3me2(s).
iJMJD6 (25 mg/kg, 50 mg/kg, i.p.) significantly suppressed the tumor growth of HeLa cell–derived xenografts and patient-derived xenograft mouse models.
iJMJD6 exhibits synergistic effects on tumor growth when combined with BRD4 inhibitor JQ1 and ERα degrader fulvestrant.

物理化学性质&存储条件

分子量 277.283
分子式 C16H11N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(1H-imidazo[4,5-c]pyridin-2-yl)-6-methyl-2H-chromen-2-one

参考文献

1. Rong-Quan Xiao, et al. Proc Natl Acad Sci U S A. 2022 Aug 23;119(34):e2200753119.

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