Talmapimod

SKU: orb1309113

Description

Talmapimod (SCIO-469) is a potent, orally bioavailable, and highly selective ATP-competitive inhibitor of p38α MAP kinase (IC50 = 9 nM). It demonstrates significant selectivity over p38β and other kinases. This compound has been utilized in research to investigate p38α's role in inflammatory pathways in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 309913-83-5
• MW: 513
• Purity: 98.00% (May vary between batches)
• Formula: C₂₇H₃₀ClFN₄O₃
• SMILES: C[C@H]1CN([C@H](C)CN1Cc1ccc(F)cc1)C(=O)c1cc2c(cn(C)c2cc1Cl)C(=O)C(=O)N(C)C
• Target: p38 MAPK
• Solubility: DMSO:95 mg/mL (185.19 mM)

Bioactivity

• Target IC50:
  p38β:90 nM|p38α:9 nM
• In Vivo:
  Talmapimod (SCIO-469), targeting p38α MAPK, reduces myeloma burden and prevents myeloma bone disease. In 5T2MM and 5T33MM models, it inhibits multiple myeloma growth and bone diseases. Administered at 10-90 mg/kg orally, twice daily for 14 days, Talmapimod dose-dependently diminishes tumor growth and decreases the weight of palpable tumors at termination.
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• In Vitro:
  phosphorylation of p38 MAPK inhibited by Talmapimod (100-200 nM; 1 hour) in MM cells.In human whole blood, LPS-induced TNF-a production inhibited by Talmapimod . Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
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Storage & Handling

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

Alternative Names

cells, cytotoxicity, Hsp27, Inhibitor, inhibit, myeloma, multiple, p38 MAPK, p38α, p38β, p38MAPK, phosphorylation, Talmapimod, SCIO 469, SCIO469, SCIO-469, tumor

Compound Identifiers

PubChem CID

9871074