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Chemical Structure : BSJ-04-122
CAS No.: 2513289-74-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $598 | In stock | |
| 100 mg | $958 | In stock | |
| 250 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 313.745 | |
| Formula | C15H12ClN5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(2-((5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)phenyl)acrylamide |
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1. Jie Jiang, et al. Cell Chem Biol. 2020 Dec 17;27(12):1553-1560.e8.
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