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KDM2A/7A-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KDM2A/7A-IN-1图片
CAS NO:2169272-46-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
KDM2A/7A-IN-1 是一种首创、选择性、细胞通过性的组蛋白赖氨酸去甲基化酶 KDM2A/7A 抑制剂,对 KDM2A 的 IC50 值为 0.16?μM,对其选择性是对其他 JmjC 赖氨酸去甲基化酶的 75 倍,同时对甲基转移酶和组蛋白乙酰转移酶无作用。
Cas No.2169272-46-0
Canonical SMILESCC(N([C@@H](C1=CN=CC(CCCCCCCN2CCCC2)=C1)[C@@]3(C4=CC=CC=C4)C#N)C5=C3C=CC=C5)=O
分子式C33H38N4O
分子量506.68
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases[1]. IC50: 0.16 μM (KDM2A)[1]

KDM2A/7A-IN-1 ((S,S)-6) is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive to methyl transferases, and histone acetyl transferases[1].KDM2A/7A-IN-1 (0.4, 3.1, 6.2 μM) augments cellular H3K36me2 levels in HeLa cells ectopically expressing catalytically active KDM2A[1].

[1]. Gerken PA, et al. Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7. Angew Chem Int Ed Engl. 2017 Dec 4;56(49):15555-15559.