MK2 Inhibitor III (MK2-IN-3) is an ATP-competitive MK2 (MAPKAP-K2) inhibitor with an IC50 value of 8.5 nM. MK2-IN-3 inhibits TNFα production in U937 cells, with IC50 of 4.4 μM, respectively. MK2-IN-3 (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model.
| Molecular Weight | 340.38 |
| Formula | C21H16N4O |
| CAS Number | 724711-21-1 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage | -20°C, protect from light |
| 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.
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| BSJ-04-122
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. |
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