An inhibitor of p38α MAPK (IC50 = 0.016 µM); selective for p38α over p38β

SD-06 – 10 mg

Brand:
Cayman
CAS:
271576-80-8
Storage:
-20
UN-No:
Non-Hazardous - /

SD-06 is an ATP-competitive inhibitor of p38α MAPK (IC50 = 0.016 µM).{54326} 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.  

 

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SKU: 30686 - 10 mg Category:

Description

An inhibitor of p38α MAPK (IC50 = 0.016 µM); 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); 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); decreases IL-1β-induced production of PGE2 in patient-derived RASFs (IC50 = 96.2 nM); reduces carrageenan-induced paw swelling and hyperalgesia in rats at 30 mg/kg; reduces the incidence of arthritis in a mouse model of collagen-induced arthritis; 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

Synonyms:  SD-006

Molecular weight: 397.9

CAS: 271576-80-8

Purity: ≥98%

Formulation: A solid

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