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 제품안내  분자생물학   Protein Research  Protein Kinase Research

TGF-β Signaling Inhibitors

TGF-β ligand는 serine/thereonine kinase인 Type Ⅰ과 Type Ⅱ 수용체에 결합하여 신호를 전달하여 핵내의 표적유전자를 활성화 시키며, 암을 유발합니다.

TGF-β Signaling에서 TGF-β receptor Kinase의 작용을 억제하는 inhibitor를 소개합니다.
Merck Millipore
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  • TGF-β Recepptor Kinase Inhibitors
    Cat. No. Name Product Biological Activity
    566405 Smad3 Inhibitor, SIS3 6,7-Dimethoxy-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinoline, Specific Inhibitor of Smad3, SIS3 Selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling
    616456 TGF-β RI Kinase Inhibitor V Transforming Growth Factor-β Type I Receptor Kinase Inhibitor V, 2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine, SD-208, ALK5 Inhibitor V Acts as a potent, selective, and reversible inhibitor of TGF-β RI/ALK5 kinase (EC50 = 48 nM).
    616451 TGF-β RI Kinase Inhibitor [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, LY-364947, HTS-466284 Acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β Receptor I kinase (IC50 = 51 nM).
    616453 TGF-β RI Kinase Inhibitor III Transforming Growth Factor-β Type I Receptor Kinase Inhibitor III, 2-(5-Benzo[1,3]dioxol-4-yl-2-tert-butyl-1H-imidazol-4-yl)-6-methylpyridine, HCl, ALK5 Inhibitor III Acts as a potent, ATP-competitive, reversible, and selective inhibitor of activin receptor-like kinase 4 (IC50 = 129 nM), 5 ( IC50 = 47 nM), and 7.
    616454 TGF-β RI Kinase Inhibitor IV Transforming Growth Factor-β Type I Receptor Kinase Inhibitor IV, 3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole, A-83-01, ALK5 Inhibitor IV Selectively inhibit ALK-4/5/7-mediated (IC50 = 45, 12, and 7.5 nM, respectively, in luciferase transcription activity assays), but not ALK-1/2/3/6-mediated cellular signaling in Mv1Lu R4-2 transfectants expressing the individual Type I TGF-β receptors
    616458 TGF-β RI Kinase Inhibitor VII 1-(2-((6,7-Dimethoxy-4-quinolyl)oxy)-(4,5-dimethylphenyl)-1-ethanone, ALK5 Inhibitor VII Acts a potent ATP-competitive inhibitor of ALK5/TGF-β Receptor I kinase activity (IC50 = 0.63 uM), while inhibiting c-Src only at higher concentrations (IC50 = 13 uM).
    616459 TGF-β RI Kinase Inhibitor VIII 6-(2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl)-quinoxaline, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor VIII, SB-525334, ALK5 Inhibitor VIII Acts as a potent, highly selective, ATP-competitive inhibitor against type I TGF-β receptor TβR-I/ALK5 (IC50 = 14.3 nM), while exhibiting 4-fold less potency toward ALK4 (IC50 = 58.5 nM) and little or no activity against ALK2/3/6 and a panel of 26 other commonly studied kinases (≤29% inhibition at 10 uM).