Pamapimod

SKU: orb1300339

Description

Pamapimod (R1503) is a selective p38 MAPK inhibitor, targeting the p38α and p38β isoforms with IC50 values of 14 nM and 480 nM, respectively. It has been utilized in preclinical research to investigate p38's role in inflammatory diseases, with studies demonstrating its effects in both cellular assays and animal models of arthritis.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 449811-01-2
• MW: 406.38
• Purity: 97.63% (May vary between batches)
• Formula: C₁₉H₂₀F₂N₄O₄
• SMILES: Cn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O
• Target: p38 MAPK,Autophagy
• Solubility: DMSO:45 mg/mL (110.73 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:27 mg/mL (66.44 mM)

Bioactivity

• Target IC50:
  p38α:0.014 ±0.002μM|p38β:0.48±0.04 μM
• In Vivo:
  In murine collagen-induced arthritis, pamapimod reduced Clinicalal signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod.
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• In Vitro:
  Pamapimod inhibited p38, but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients.
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Storage & Handling

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

Alternative Names

Autophagy, anti-inflammation, inhibit, IL-1β, IL-6, Inhibitor, JNK, Pamapimod, LPS, p38 MAPK, p38MAPK, p38α, p38β, R 1503, R1503, R-1503, TNF-α, Ro4402257, Ro-4402257, Ro 4402257

Compound Identifiers

PubChem CID

16220188