MKC3946CAS号: 1093119-54-0分子式: C21H20N2O3S分子量: 380.46描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO : 20 mg/mL (52.57 mM; Need ultrasonic)
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生物活性 | |
靶点 |
IRE1α endoribonuclease
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In vitro(体外研究) |
MKC-3946 triggers modest growth inhibition in MM cell lines, without toxicity in normal mononuclear cells. Importantly, it significantly enhances cytotoxicity induced by bortezomib or 17-AAG, even in the presence of bone marrow stromal cells or exogenous IL-6. Both bortezomib and 17-AAG induce ER stress, evidenced by induction of XBP1s, which is blocked by MKC-3946. Apoptosis induced by these agents is enhanced by MKC-3946, associated with increased CHOP. MKC-3946 treatment does not inhibit IRE1α kinase function or binding of activated IRE1α to TRAF2 and downstream JNK signaling.
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In vivo(体内研究) |
MKC-3946 inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells.
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分子结构图