An inhibitor of p38α MAPK
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SD-06

Item No. 30686

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $229

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    25 mg

    $418

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    50 mg

    $655

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    Product Description

    SD-06 is an ATP-competitive inhibitor of p38α MAPK (IC50 = 0.016 µM).1 It is selective for p38α over p38β, p38γ, and p38δ 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-α, IL-6, and IL-1β release from primary human monocytes (IC50s = 79.4, 106.9, and 105.9 nM, respectively). It decreases IL-1β-induced production of prostaglandin E2 (PGE2; Item No. 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burnette, B.L., Selness, S., Devraj, R., et al. SD0006: A potent, selective and orally available inhibitor of p38 kinase. Pharmacology 84(1), 42-60 (2009).