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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1093119-54-0
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥2200.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥666.0 |
| 规格: | 5 mg | 产品价格: | ¥2000.0 |
| 规格: | 10 mg | 产品价格: | ¥3146.0 |
| 规格: | 25 mg | 产品价格: | ¥5663.0 |
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MKC3946
CAS No. : 1093119-54-0
MCE 国际站: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.
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