|2-羟基-6-(5-(4-甲基哌嗪-1-羰基)噻吩-2-基)-1-萘甲醛|CsnPharm

CAS No.: 1093119-54-0

MKC3946 Catalog No. CSN18840

Synonyms: MKC3946

MKC3946 is a small-molecule IRE1α endoribonuclease domain inhibitor which can block XBP1 splicing.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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].
动物研究
剂量
Mice: 100 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 100 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Mimura N, Fulciniti M, et al. Blockade of XBP1 splicing by inhibition of IRE1α is a promising therapeutic option in multiple myeloma. Blood. 2012 Jun 14;119(24):5772-81.
[2] Mimura N, Fulciniti M, Gorgun G, Tai YT, Cirstea D, Santo L, Hu Y, Fabre C, Minami J, Ohguchi H, Kiziltepe T, Ikeda H, Kawano Y, French M, Blumenthal M, Tam V, Kertesz NL, Malyankar UM, Hokenson M, Pham T, Zeng Q, Patterson JB, Richardson PG, Munshi NC, Anderson KC. Blockade of XBP1 splicing by inhibition of IRE1α is a promising therapeutic option in multiple myeloma. Blood. 2012 Jun 14;119(24):5772-81. doi: 10.1182/blood-2011-07-366633. Epub 2012 Apr 26. PMID: 22538852; PMCID: PMC3382937.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6284 mL
- 13.1420 mL
- 26.2840 mL
- 5 mM
- 0.5257 mL
- 2.6284 mL
- 5.2568 mL
- 10 mM
- 0.2628 mL
- 1.3142 mL
- 2.6284 mL

技术信息

CAS号

1093119-54-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H20N2O3S

运输

蓝冰

分子量

380.46

别名

MKC3946

溶解度

DMSO	30.0 mg/mL (78.9 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

MKC3946 Catalog No. CSN18840

靶点选择性

请登录您的专属账户

确认信息