A potent

Pamapimod – 1 mg

Brand:
Cayman
CAS:
449811-01-2
Storage:
-20
UN-No:
Non-Hazardous - /

Pamapimod is a potent inhibitor of p38α MAP kinase (IC50 = 14 nM).{33190} It displays over 30-fold selectivity for p38α over p38β, has no activity against p38δ or p38γ, and has limited activity against a panel of 350 other kinases. Pamapimod blocks LPS-induced TNF-α production by monocytes and IL-1β generation in whole blood, and it inhibits spontaneous TNF-α release from synovial explants from patients with rheumatoid arthritis.{33191,33189} It is orally bioavailable and abrogates inflammation and bone loss in an animal model of arthritis and pain in a rat model of hyperalgesia.{33191} Pamapimod suppresses the expression of inflammation-associated genes in primary, IL-1β-stimulated human chondrocytes.{33192}  

 

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Description

A potent, selective inhibitor of p38α MAPK (IC50 = 14 nM); blocks inflammatory signaling in cells, whole blood, and synovial explants; orally bioavailable, abrogating inflammation, bone, and pain in animal models

Formal name: 6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one

Synonyms:  R 1503|Ro 4402257

Molecular weight: 406.4

CAS: 449811-01-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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