SB220025

SKU: orb1699391

Description

SB220025 is a potent, orally bioavailable, and selective p38 MAPK inhibitor that also suppresses p56Lck and PKC activity. It disrupts endothelial growth hormone-induced calcium signaling and angiogenesis, making it a valuable compound for studying inflammatory diseases such as arthritis in both cellular and animal models.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 165806-53-1
• MW: 338.38
• Purity: 99.97% (May vary between batches)
• Formula: C₁₈H₁₉FN₆
• SMILES: FC1=CC=C(C=C1)C=2N=CN(C2C=3N=C(N=CC3)N)C4CCNCC4
• Target: Src,PKC,p38 MAPK
• Solubility: DMSO:100 mg/mL (295.53 mM)

Bioactivity

• Target IC50:
  p38 MAPK (human):60 nM|PKC:2.89 µM|p56Lck:3.5 µM
• In Vivo:
  A single oral dose of 3-50 mg/kg SB220025 inhibited the production of inflammatory cytokines in vivo . Intraperitoneal administration of 5, 30, and 50 mg/kg SB220025 in a double dose inhibited angiogenesis in a mouse model of air sac granuloma . Oral administration of 30 mg/kg SB220025, given as a double dose for 3, 5, 7, or 14 days prevented the increase in angiogenesis after day 3 in the mouse air sac angiogenesis model . Oral administration of 50 mg/kg SB220025, double-dosed for 10 days, effectively inhibited the progression of arthritis in a chronic inflammatory disease model .
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• In Vitro:
  SB220025 is an ATP-competitive and selective inhibitor of human p38 MAPK with an IC50 of 60 nM. p56Lck and PKC were also inhibited by SB220025 with IC50s of 3.5 and 2.89 µM, respectively. SB220025 (20 μM; 6 h) significantly reduced IL-8 gene expression in HUVEC cells in response to globular adiponectin (gAd).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB 220025, SB220025, SB-220025

Compound Identifiers

PubChem CID

5164