A 83-01 is a selective inhibitor of TGF-b type I receptor. A 83-01 treatment increases tumor permeability. A 83-01 is an inhibitor of TGF-beta type I receptor kinase (ALK5), activin type IB receptor (ALK4), and nodal type I receptor (ALK7) (IC50s = 12, 45, and 7.5nM, respectively).1 It blocks the phosphorylation of SMAD2/3 and inhibits TGF-beta-induced epithelial-to-mesenchymal transition. It has little effect on bone morphogenic type I receptors, p38 mitogen-activated protein kinase, or ERK.1 A 83-01 has been used to reprogram fibroblasts into alternative lineages, including neural stem cells and cardiomyocytes. Synonyms: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, TGF-beta RI Kinase Inhibitor IV, Transforming Growth Factor-beta Type I Receptor Kinase Inhibitor IV, 3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole, ALK5 Inhibitor IV CAS No: 909910-43-6 Molecular Formula: C25H19N5S Molecular Weight: 421.52 Appearance: Off-white to pale yellow powder Purity (HPLC): 95% Melting Point: 207-209C Method for Determining Identity: Proton NMR Spectroscopic Analysis and Mass Spectrum Analysis lambdamax: 227, 307nm Solubility: Ethanol: 0.3mg/ml, DMSO: 14mg/ml, DMF: 25mg/ml, DMSO:PBS (pH 7.2) (1:2): (0.3mg/ml) Storage and Stabillity: Store at -20C under inert atmosphere. Hygroscopic. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molecular Weight:
421.52
Purity:
95%
Form:
Off-white to pale yellow powder
CAS Number:
[909910-43-6]
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