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MKC3946

CAS No. : 1093119-54-0

MCE 站：MKC3946

产品活性：MKC3946 是一种有效的 IRE1α 抑制剂，常用于癌症研究。

研究领域：Cell Cycle/DNA Damage

作用靶点：IRE1

In Vitro: MKC-3946 blocks?XBP1?mRNA splicing and exhibits cytotoxicity against AML cells. MKC-3946 inhibits XBP1S expression induced by tunicamycin (TM) in NB4 cells (B) and AML sample from patients. MKC-3946 prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production. MKC-3946 is an IRE1α endoribonuclease domain inhibitor that blocks XBP1 mRNA splicing and triggers modest growth inhibition in MM cells. MKC-3946 inhibits XBP1s expression induced by Tm in a dose-dependent manner, but does not affect phosphorylation of IRE1α. MKC-3946 blocks XBP1 splicing and enhances cytotoxicity induced by bortezomib or 17-AAG. MKC-3946 (10μM) enhances ER stress-mediated apoptosis induced by bortezomib or 17-AAG, and enhances cytotoxicity of ER stressors, even in the presence of BMSCs or exogenous IL-6.

In Vivo: MKC-3946 (100 mg/kg, i.p.) inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells, alone or with bortezomib. MKC-3946 significantly reduces MM tumor growth in the treatment versus control group. Inhibition of XBP1 splicing by MKC-3946 is associated with decreased MM growth in vivo, alone or in combination with bortezomib.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Endoplasmic Reticulum Stress Compound Library  |  Sunitinib  |  4μ8C  |  STF-083010  |  Kira8  |  Toyocamycin  |  6-Bromo-2-hydroxy-3-methoxybenzaldehyde  |  3,6-DMAD hydrochloride  |  KIRA-7

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