127 products were found matching "K04674"!

SB-431542 is a potent and selective inhibitor of the TGF-beta1 receptor ALK5 (IC50 = 94 nM). It is a less potent antagonist of ALK4 (IC50 = 140 nM) and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB-431542 specifically blocks Smad signaling, reducing gene...

ALK5 inhibitor II is a cell permeable, selective inhibitor of the TGF-beta type 1 activin like kinase receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-beta cellular assay, and ALK5 binding in HepG2 cells, respectively). This inhibitor demonstrated less potent activity (IC50s > 16 µM) when...

transforming growth factor beta receptor 1 (TGFBR1), a key stimulator of tumor proliferation and metastasis, was a direct target of miR-98-5p. miR-98-5p overexpression resulted in the downregulation of TGFBR1 and the suppression of the viability, proliferation, migration and invasion of A549 and H1299 cells.

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 7.5 nM, respectively). It blocks the phosphorylation of SMAD2/3 and inhibits TGF-beta-induced epithelial-to-mesenchymal transition. It has little effect on bone...

LY2157299 is a small molecule inhibitor of the TGF-beta receptor type 1 kinase (IC50 = 56 nM). It has been used to study the role of TGF-beta signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts. LY2157299 has also been shown to inhibit the...

IN 1130 is an inhibitor of activin receptor-like kinase 5 (ALK5), also known as TGF-beta receptor type 1 (TGF-betaRI, IC50 = 5. nM). It is selective for ALK5 over a panel of 27 other kinases at 5 µM. IN 1130 (10 mg/kg per day) decreases renal fibrogenesis, inflammatory cell infiltration, and tubular atrophy in a...

SB-431542 inhibits activin receptor-like kinases ALK4, ALK5, and ALK7, this inhibition leads to inhibition of activin and TGF- signaling with no downstream effects on ERK, JNK, or MAPK. SB-431542 exhibits anti-angiogenic and anticancer activity. In vitro, SB-431542 inhibits proliferation and motility of glioma...

LY2157299 is a small molecule inhibitor of the TGF-beta receptor type 1/type II kinases (IC50 = 69 nM). It has been used to study the role of TGF-beta signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 µM of the compound completely disrupts Smad-2 phosphorylation, an immediate...

Transforming growth factor-beta (TGF-beta) signals through a cell surface heteromeric complex involving type I (TGF-beta RI) and type II (TGF-beta RII) receptors. Downstream signal transduction is mediated by the TGF-beta RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective...

ALK5 inhibitor II is a cell permeable, selective inhibitor of the TGF-beta type 1 activin like kinase receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-beta cellular assay, and ALK5 binding in HepG2 cells, respectively). This inhibitor demonstrated less potent activity (IC50s > 16 µM) when...

SB-505124 inhibits the TGF-beta1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and...

ALK5 (activin-like) antagonist.