BMS582949

SKU: orb1300464

Description

BMS-582949 is a selective p38 MAPK inhibitor with an IC50 of 13 nM, effectively blocking both the kinase and its activation. This compound is a valuable research tool for investigating p38-mediated pathways in inflammatory and autoimmune disease models, applicable in both cellular and animal studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 623152-17-0
• MW: 406.48
• Purity: 98.43% (May vary between batches)
• Formula: C₂₂H₂₆N₆O₂
• SMILES: N(C=1C=2N(C=C(C(NCCC)=O)C2C)N=CN1)C3=CC(C(NC4CC4)=O)=CC=C3C
• Target: p38 MAPK
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:75 mg/mL (184.51 mM)

Bioactivity

• Target IC50:
  p38 MAPK (cell-free assay):13 nM
• In Vivo:
  The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.
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• In Vitro:
  BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop.
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Storage & Handling

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

Alternative Names

p38MAPK, p38 MAPK, PS 540446, PS540446, PS-540446, BMS 582949, BMS582949, BMS-582949

Compound Identifiers

PubChem CID

10409068