TGF-βR1(ALK5)

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.

TGF-βR1(ALK5) 相关产品（6）

货号	产品名	Cas	产品描述
PC15925	A 77-01	607737-87-1	强效ALK5抑制剂，A 77-01是TGF-β I型受体超家族ALK5抑制剂，IC50为25 nM。
PC15926	A 83-01	909910-43-6	ALK-5抑制剂，A 83-01 是有效的 ALK5，ALK4 和 ALK7 的抑制剂， IC50 值分别为 12，45 和 7.5 nM。
PC15990	ALK5 Inhibitor II (hydrochloride)		ALK5抑制剂，IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively，ALK5 Inhibitor II is an ALK5 inhibitor.
PC15940	GW788388	452342-67-5	ALK5抑制剂，GW788388 是一种有效的 ALK5 抑制剂，IC50 值 18 nM；同时抑制 TGF-β II 型受体和激活素 II 型受体的活性，但对 BMP II 型受体无作用。
PC15935	SB-505124 hydrochloride	356559-13-2	TGF-β/活化素信号传导中ALK5/ALK4/ALK7 的抑制剂，SB-505124 hydrochloride 是一种选择性的 TGFβR 抑制剂，对 ALK4，ALK5 的 IC50 值分别为 129 nM 和 47 nM。
PC15936	SD-208	627536-09-8	TGF-βR I激酶抑制剂，SD-208 是一种选择性的 TGF-βRI (ALK5) 抑制剂，IC50 值为 48 nM，对其选择性是对 TGF-βRII 的 10 倍。