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抑制剂/激活剂

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凋亡与自噬

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GSK126 GSK2816126A

GSK126 (GSK2816126A, GSK2816126) 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。

货号：
TK0286
规格：

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1346574-57-9
生物活性	GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
分子式	C31H38N6O2
分子量	526.67
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 12.5 mg/mL (23.73 mM; Need ultrasonic)
体内研究	GSK126 is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight in female beige SCID mice. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.
体外研究	GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki=0.5-3 nM) independent of substrate used, and is competitive with S-adenosyl-methionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes (EZH1, IC50=680 nM). Treatment of three SCLC cell lines with GSK126, induces growth inhibition. SCLC cell lines (Lu130, H209, and DMS53) are treated with 0.5, 2, and 8 μM GSK126, and growth curve is analyzed by WST-8 assay. Inhibition of cellular growth by GSK126 treatment is observed at 8 μM in all the three cell lines, while Lu130 and H209 are more sensitive to GSK126, even at lower doses.
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纯度及产品资料	98%

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