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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-JG-2016
JG-2016

Chemical Structure : JG-2016

CAS No.: 2887480-87-5

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JG-2016 (JG2016)

货号: PC-49533Not For Human Use, Lab Use Only.

JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays.

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5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥6580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays.
JG-2016 binds HAT1 at the cofactor-binding site and does not compete with the histone substrate.
JG-2016 robustly inhibited cell growth (EC50=10.4 uM) in triple-negative breast cancer cell line HCC1806, inhibits A549 (lung cancer) with EC50 of 1.9 uM.
JG-2016 (50-100 mg/kg, i.p.) impairs HAT1 dependent acetylation and suppresses tumor growth with minimal toxicity in vivo.

物理化学性质&存储条件

分子量 376.841
分子式 C18H21ClN4O3
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

7-chloro-8-ethyl-10-(2-isobutoxyethyl)benzo[g]pteridine-2,4(3H,10H)-dione

参考文献

1. Gaddameedi JD, et al. J Med Chem. 2023 Apr 27;66(8):5774-5801.

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