SD-06

SD-06 is an ATP-competitive inhibitor of p38alpha MAPK (IC50 = 0.016 µM). It is selective for p38alpha over p38beta, p38gamma, and p38delta MAPKs (IC50s = 0.677, >100, and >100 µM, respectively), as well as a panel of 54 additional kinases (IC50s = >3 µM for all). SD-06 inhibits LPS-induced TNF-alpha, IL-6, and IL-1beta release from primary human monocytes (IC50s = 79.4, 106.9, and 105.9 nM, respectively). It decreases IL-1beta-induced production of prostaglandin E2 (PGE2, Cay-14010) in patient-derived rheumatoid arthritis synovial fibroblasts (RASFs, IC50 = 96.2 nM). SD-06 (30 mg/kg) reduces carrageenan-induced paw swelling and hyperalgesia in rats. It also reduces the incidence of arthritis in a mouse model of collagen-induced arthritis and protects against joint and bone destruction in a rat model of streptococcal cell wall-induced arthritis.Formal Name: 1-[4-[5-(4-chlorophenyl)-4-(4-pyrimidinyl)-1H-pyrazol-3-yl]-1-piperidinyl]-2-hydroxy-ethanone. CAS Number: 271576-80-8. Synonyms: SD-006. Molecular Formula: C20H20ClN5O2. Formula Weight: 397.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 240, 282 nm. SMILES: O=C(CO)N(CC1)CCC1C2=NNC(C3=CC=C(Cl)C=C3)=C2C4=NC=NC=C4O=C(CO)N(CC1)CCC1C2=NNC(C3=CC=C(Cl)C=C3)=C2C4=NC=NC=C4. InChi Code: InChI=1S/C20H20ClN5O2/c21-15-3-1-13(2-4-15)19-18(16-5-8-22-12-23-16)20(25-24-19)14-6-9-26(10-7-14)17(28)11-27/h1-5,8,12,14,27H,6-7,9-11H2,(H,24,25). InChi Key: CATQHDWESBRRQA-UHFFFAOYSA-N.