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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-BSJ-04-122
BSJ-04-122

Chemical Structure : BSJ-04-122

CAS No.: 2513289-74-0

BSJ-04-122

货号: PC-38277Not For Human Use, Lab Use Only.

BSJ-04-122 is a potent, selective, covalent dual MKK4/7 inhibitor with IC50 of 4/181 nM, displays excellent kinome selectivity.

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5 mg ¥780 In stock
10 mg ¥1180 In stock
25 mg ¥1980 In stock
50 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BSJ-04-122 is a potent, selective, covalent dual MKK4/7 inhibitor with IC50 of 4/181 nM, displays excellent kinome selectivity.
BSJ-04-122 covalently targets a conserved cysteine (Cys247 for MKK4, and Cys261 for MKK7) located before the DFG motif.
BSJ-04-122 exhibits potent cellular target engagement and induces robust target-specific downstream effects.
In breast cancer cell lines, BSJ-04-122 potently inhibited JNK phosphorylation, BSJ-04-122 significantly decreased levels of T183/Y185 pJNK at 5 uM, resulting in complete inhibition at 10 uM in MDA-MB-231 cells.
The combination of the dual MKK4/7 inhibitor BSJ-04-122 with a selective, covalent JNK inhibitor (JNK-IN-8) demonstrated an enhanced antiproliferative activity against triple-negative breast cancer cells.

物理化学性质&存储条件

分子量 313.745
分子式 C15H12ClN5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-((5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)phenyl)acrylamide

参考文献

1. Jie Jiang, et al. Cell Chem Biol. 2020 Dec 17;27(12):1553-1560.e8.

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