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TGF-beta/Smad

As a founding member of the largest family of secreted morphogens in mammals, transforming growth factor β (TGF-β) can induce anchorage-independent growth. There are four subclasses of the TGF-β family with different biological functions. After transmembrane serine/threonine kinases binding form a heteromeric complex of type I and II receptors, TGF-β signaling pathway is activated. Smad signaling pathway is activated after the phosphorylation of the type I receptor by the type II kinase. In the eponymous TGF-β pathway, this occurs via ligand-induced cooperative assembly of the receptor complex. There are so many important targets related to Smad including HDAC1, Notch, STAT3, ERK and p38.  [show the full text]

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S1067 SB 431542 SB 431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM. (3)
S2230 LY2157299 LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.
S2618 LDN193189 LDN193189 is a selective inhibitor of ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. (1)
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively.
S1476 SB 525334 SB 525334 is a potent and selective inhibitor of TGF-β1 (ALK5) with IC50 of 14.3 nM. (8)
S2907 Pirfenidone Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells.
S2186 SB-505124 SB505124 is a selective inhibitor of ALK4 and ALK5 with IC50 of 129 nM and 47 nM, respectively.
S2750 GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM.
S2805 LY364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM.

TGF-beta/Smad

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