TGF beta Receptor (TGFBR)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.

The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.

Cat. No.	Product Name	CAS No.	Information
H9097	Lingzhifuran A	2186652-58-2	Lingzhifuran A is a potent Smad3 phosphorylation inhibitor.
H7616	VU 0364849	1206711-14-9	A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM; also inhibits ALK6 (Ki<1 nM) and ALK2 (Ki=42.77 nM), little to no affinity for ALK4/5, BMPR2, AMPK etc.; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.
H7615	TP-0427736	864374-00-5	TP-0427736 (TP0427736) is a novel potent and selective ALK5 inhibitor with IC50 of 2.72 nM, displays 300-fold selecitvity over ALK3; inhibits Smad2/3 phosphorylation in A549 cells (IC50=8.7 nM) and decreases the growth inhibition of human outer root sheath cells; significantly decreases Smad2 phosphorylation in mouse skin after topical application, may serves as a potential new therapy for AGA.
H7614	TASP0382088	1253941-85-3	A potent, selective ALK5 inhibitor with IC50 of 4.8 nM, >100-fold selectivity over 95 different kinases; inhibits TGF-β-induced Smad2/3 phosphorylation at cellular level with IC50 of 17 nM, inhibits Smad2 phosphorylation in mouse skin after topical application.
H7613	SD-208	627536-09-8	SD-208 is a potent, selective TGF-β receptor I kinase (TGF-βRI) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII kinase and >20-fold over a panel of related protein kinases; inhibits the growth inhibition of TGF-beta-sensitive CCL64 cells mediated by recombinant TGF-β1 or TGF-β2 or of TGF-β-containing glioma cell supernatant with EC50 of 0.1 uM; inhibits constitutive and TGF-β–induced invasion of glioma cells, inhibits TGF-β signaling in immune effector cells; blocks TGF-β signaling in the brain and inhibits the growth of syngeneic SMA-560 experimental gliomas in vivo.
H7612	SB-431542	301836-41-9	SB-431542 is a potent, specific TGF-β type I receptor (ALK5) inhibitor with IC50 of 94 nM; also substantially inhibits ALK4 and 7, but not other ALKs; efficiently inhibits the ability of activated ALK4, ALK5, and ALK7 to phosphorylate Smad2; a selective inhibitor of endogenous activin and TGF-beta signaling but has no effect on BMP signaling, and has no effect on components of the ERK, JNK, or p38 MAP kinase pathways.
H7611	SB 525334	356559-20-1	SB 525334 is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM); blocks TGFβ1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibits TGFβ1-induced increases in PAI-1 and procollagen α1 mRNA expression in A498 renal epithelial carcinoma cells at 1 uM; significantly inhibits PAN-induced proteinuria in rat model of nephritis-induced renal fibrosis.
H7610	San78-130	66018-45-9	San78-130 is a potent, selective activin receptor-like Kinase 1 (ALK1) inhibitor with IC50 of 62 nM, with greater selectivity compared with L-783277; inhibits (>80%) only 6 kinases including ALK1, FLT3, FLT4, KDR, MEK2 and MKK6 in a panel of 342 kinases, shows weak inhibition for other ALK isotypes; suppresses the BMP9-induced Smad1/5 pathway by mainly inhibiting ALK1 in C2C12 cells, promotes angiogenesis in both endothelial tube formation and microfluidic chip based 3D angiogenesis assays
H7609	RepSox	446859-33-2	RepSox (E-616452, SJN-2511) is a potent, selective inhibitor of TGF-β type I receptor ALK5 with Ki of 25 nM, inhibits ALK5 autophosphorylation with IC50 of 4 nM, can replace the central reprogramming factor Sox2 by inducing nanog; specifically acts by inhibiting Tgf-β signaling, does not act by inducing Sox2 expression in the target fibroblasts; efficiently replaces transgenic Sox2 in the absence of VPA and c-Myc, as well as in both embryonic and adult fibroblasts; demonstrates effectivity at generating iPSCs.
H7608	R-268712	879487-87-3	R-268712 is a potent, selective, orally active inhibitor of TGF-β type I receptor ALK5 with IC50 of 2.5 nM, >5,000-fold more selectivity than p38 MAPK; inhibits the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model at doses of 1, 3 and 10mg/kg, also reduces proteinuria and glomerulosclerosis significantly with improvement of renal function in glomerulonephritis models.

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