A potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM

FR180204 – 25 mg

Brand:
Cayman
CAS:
865362-74-9
Storage:
-20
UN-No:
Non-Hazardous - /

FR180204 is a potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively).{25542} It is much less effective against p38α (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases.{25542} FR180204 blocks ERK-mediated signaling from TGF-β to AP-1 (IC50 = 3.1 μM).{25542} It attenuates delayed-type hypersensitivity in collagen-immunized mice and ameliorates collagen-induced arthritis in mice.{25543}  

 

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Description

A potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively); much less effective against p38α (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases; blocks ERK-mediated signaling from TGF-β to AP-1 (IC50 = 3.1 μM)

Formal name: 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine

Synonyms:  ERK Inhibitor II

Molecular weight: 327.3

CAS: 865362-74-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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