BSJ-04-122
Modify Date: 2024-01-06 22:06:12
BSJ-04-122 structure
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Common Name | BSJ-04-122 | ||
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| CAS Number | 2513289-74-0 | Molecular Weight | 313.745 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C15H12ClN5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of BSJ-04-122BSJ-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.SJ-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. |
| Name | BSJ-04-122 |
|---|
| Description | 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.SJ-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. |
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| References | 1. Jie Jiang, et al. Cell Chem Biol. 2020 Dec 17;27(12):1553-1560.e8. |
| Molecular Formula | C15H12ClN5O |
|---|---|
| Molecular Weight | 313.745 |