YUKA1 是一种有效、可透过细胞的赖氨酸脱甲基化酶 (KDM5A) 抑制剂，IC50 值为 2.66 μM，对 KDM5C 的作用较弱，IC50 值为 7.12 μM，对 KDM5B，KDM6A 或 KDM6B 无作用。YUKA1 可增加人细胞中 H3K4me3 的水平，具有抗肿瘤活性。
CAS：708991-09-7
分子式：C13H16N4O2S
分子量：292.36
纯度：98%
存储：Store at -20°C

Background:

YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity[1]. IC50: 2.66 μM (KDM5A), 7.12 μM (KDM5C)[1]

[1]. Gale M, et al. Screen-identified selective inhibitor of lysine demethylase 5A blocks cancer cell growth and drug resistance. Oncotarget. 2016 Jun 28;7(26):39931-39944.