A potent inhibitor of the TGF-β receptor 1 (TGF-β R1

SB-525334 – 1 mg

Brand:
Cayman
CAS:
356559-20-1
Storage:
-20
UN-No:
Non-Hazardous - /

SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}  

 

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Description

A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals

Formal name: 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-quinoxaline

Synonyms:  TGF-β RI Kinase Inhibitor VIII

Molecular weight: 343.4

CAS: 356559-20-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ATM||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cancer|Transcription Factors||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cell Biology|Cell Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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