BSJ-04-122 is a covalent MKK4/7 dual inhibitor. BSJ-04-122 inhibits MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. BSJ-04-122 covalently targets a conserved cysteine located before the DFG motif and displays excellent kinome selectivity. BSJ-04-122 exhibits potent cellular target engagement and induces robust target-specific downstream effects. The combination of the dual MKK4/7 inhibitor with a selective, covalent JNK inhibitor demonstrated an enhanced antiproliferative activity against triple-negative breast cancer cells.
| Molecular Weight | 313.74 |
| Formula | C15H12ClN5O |
| CAS Number | 2513289-74-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Jie Jiang, et al. Cell Chem Biol. Discovery of Covalent MKK4/7 Dual Inhibitor
| Related p38 MAPK Products |
|---|
| HWY336
HWY336 is a selective, non-ATP competitive dual MKK4 and MKK7 inhibitor with IC50 values of 6 µM on MKK4 and 10 µM on MKK7 in vitro. HWY336 inhibits the phosphorylation of MKK4/MKK7 inside the activation loop or hinders the substrate to access the kinase. |
| OVA-E1 peptide TFA
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). |
| MBP MAPK Substrate
MBP MAPK Substrate is used as an exogenous substrate for MAPK. |
| OVA-E1 peptide
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). |
| EGF-R (661-681) T669 Peptide
EGF-R (661-681) T669 Peptide is a MAPK substrate that can used to measure MAPK catalytic activity. |
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