SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
| Molecular Weight | 459.58 |
| Formula | C27H33N5O2 |
| CAS Number | 2413286-32-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 125 mg/mL (ultrasonic) |
| Storage | 4°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.
[2] Sandra Röhm, et al. Eur J Med Chem. Selective targeting of the αC and DFG-out pocket in p38 MAPK
| Related p38 MAPK Products |
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| 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. |
| 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. |
| 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). |
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