MKC3946
产品说明书
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同义名 : | - |
| CAS号 : | 1093119-54-0 | |
| 货号 : | A777720 | |
| 分子式 : | C21H20N2O3S | |
| 纯度 : | 97% | |
| 分子量 : | 380.46 | |
| MDL号 : | MFCD30496700 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 18 mg/mL(47.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MKC-3946 is IRE1α endoribonuclease domain inhibitor. It inhibited basal XBP1 splicing in RPMI 8226 cells treated with tunicamycin dose-dependently at concentration<10μM post 3h, but did not affect phosphorylation of Ire1α. Consistent with downstream the inhibition of XBP1 splicing by MKC-3946, the expression of XBP1 target genes, SEC61A1, p58IPK, and ERdj4, were decreased. MKC-3946 triggered modest growth inhibition in MM cell lines and significantly enhanced cytotoxicity induced by bortezomib or 17-AAG, even in the presence of bone marrow stromal cells or exogenous IL-6. The ER stress induction by bortezomib and 17-AAG could be blocked by MKC-3946. Apoptosis induced by these agents was enhanced by MKC-3946, associated with increased CHOP. Administration of MKC-3946 at dose of 50mg/kg, i.p., inhibited XBP1 splicing in a model of ER stress induced by tunicamycin in vivo. Daily administration of MKC-3946 at dose of 100mg/kg, i.p., inhibited tumor growth in SCID mice xenograft RPMI 8226 cells and improved the survival level of the mice. Combination of MKC3946 with bortezomib could potentiated these efficiency[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.14mL 2.63mL 1.31mL |
26.28mL 5.26mL 2.63mL |
| 参考文献 |
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