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抑制剂/激活剂

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凋亡与自噬

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I-BET-762 I-BET762; GSK525762; GSK525762A

Molibresib (I-BET-762, GSK525762, GSK525762A) 是一种BET蛋白抑制剂，无细胞试验中IC50约为35 nM，抑制巨噬细胞产生促炎性蛋白质，并抑制急性炎症，对其他溴区结合域包含的蛋白具有高度选择性。

货号：
TK0290
规格：

1mg

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1260907-17-2
生物活性	Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
分子式	C22H22ClN5O2
分子量	423.9
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 : 200 mg/mL (471.81 mM; Need ultrasonic)
体内研究	The antimyeloma activity of Molibresib (I-BET 762) is tested dosed orally in an in vivo systemic xenograft model generated by injecting OPM-2 cells into NOD-SCID mice. Daily oral doses of Molibresib up to 10 mg/kg and 30 mg/kg given every other day are well tolerated with no clear impact on body weight compared with vehicle control. The plasma hLC concentration is significantly reduced in mice treated with Molibresib.
体外研究	Molibresib (I-BET 762) shows the highest affinity interaction with BET. Molibresib binds to the tandem bromodomains of BET with high affinity (dissociation constant Kd of 50.5-61.3 nM). Molibresib displaces, with high efficacy (half-maximum inhibitory concentration IC50 of 32.5-42.5 nM), a tetra-acetylated H4 peptide that had been pre-bound to tandem bromodomains of BET. Molibresib has high affinity for BD1/BD2 domain of BRD2/3/4 proteins. Molibresib treatment leads to a reduction in the recruitment of all three proteins to chromatin. Molibresib inhibits OPM-2 cell proliferation with IC50 of 60.15 nM.
文献	暂无相关参考文献
纯度及产品资料	98%

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