A potent JNK inhibitor (IC50s = 61

CC-930 – 10 mg

Brand:
Cayman
CAS:
899805-25-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).{39372} It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.  

 

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Description

A potent JNK inhibitor (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively); selective for MAP kinases; selective for JNKs over other MAPK family proteins (IC50s = 3,400 and 480 nM for p38α and ERK1, respectively); inhibits JNK in a cell lysate assay (IC50 = 200 nM); blocks phosphorylation of c-Jun in LPS-stimulated human PBMCs; inhibits TNF-α production induced by LPS when administered to rats at doses of 10 and 30 mg/kg; reduces lung fibrosis in a mouse pulmonary fibrosis model,

Formal name: trans-4-[[9-[(3S)-tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]-cyclohexanol

Synonyms:  Tanzisertib

Molecular weight: 448.4

CAS: 899805-25-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JNK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling||Research Area|Immunology & Inflammation

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