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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-ML234
ML234

Chemical Structure : ML234

CAS No.:

ML234 (ML-234)

货号: PC-22960Not For Human Use, Lab Use Only.

ML234 is a potent EZH2/LSD1 dual inhibitor with IC50 of 0.09/0.12 uM respectively, shows excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3, and 22RV1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ML234 is a potent EZH2/LSD1 dual inhibitor with IC50 of 0.09/0.12 uM respectively, shows excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3, and 22RV1.
ML234 accumulates H3K4me2 and H3K9me2 and decreases H3K27me3 in prostate cancer cells.
ML234 weakly inhibits LSD2 and MAO-A.
ML234 shows anticancer activity in all three prostate cancer cell lines (GI50s at 3.96, 1.04, and 1.63 μM).
ML234 inhibits cell migration in prostate cancer cells via a potential EMT intervention.
ML234  (80 mg/kg) daily significantly suppressed tumor volume by a tumor growth inhibitory rate (TGI) of 52.2% in 22RV1 tumor xenograft model.

物理化学性质&存储条件

分子量 726.96
分子式 C43H58N4O6
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

(±)-trans-tert-Butyl(2-(3'-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-5'-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-methyl-[1,1'-biphenyl]-4-yl)cyclopropyl)((tetrahydro-2H-pyran-4-yl)methyl)carbamate

参考文献

1. Meiling Le, et al. Journal of Medicinal Chemistry, August 28, 2024

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