KDM2A/7A-IN-1
目录号: PL15106 纯度: ≥99%
CAS No. :2169272-46-0
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中文名称
KDM2A/7A-IN-1
中文别名
化合物 T11748
英文名称
KDM2A/7A-IN-1
英文别名
KDM2A/7A-IN-1;KDM-IN-6;1H-Indole-3-carbonitrile, 1-acetyl-2,3-dihydro-3-phenyl-2-[5-[7-(1-pyrrolidinyl)heptyl]-3-pyridinyl]-, (2S,3S)-
Cas No.
2169272-46-0
分子式
C33H38N4O
分子量
506.68
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
IC50: 0.16?μM (KDM2A)
体外研究(In Vitro)
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.
KDM2A/7A-IN-1 (0.4, 3.1, 6.2 μM) augments cellular H3K36me2 levels in HeLa cells ectopically expressing catalytically active KDM2A. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 200 mg/mL (394.73 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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