Single pass serine/threonine kinase receptors are TGF-Rs, or transforming growth factor receptors. Transforming growth factor beta (TGF-beta) is a pleiotropic cytokine that participates in a wide range of biological functions, including the regulation of growth, differentiation, migration, cell survival, adhesion, and the specification of developmental fate, in both healthy and pathological conditions. Members of the TGF-beta superfamily communicate via a receptor complex made up of type II and type I receptors, both of which are serine/threonine kinases.At the center of the signaling cascade, the type I receptors, also known as activin receptor-like kinases (ALK), transmit TGF-beta signals to Smad proteins, which are intracellular transcriptional regulators.
ALKs have extracellular binding domains, transmembrane domains, GS domains that type II receptors use to activate them, and kinase domains that trigger the activation of subsequent 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. ALKs may make good drug targets because they have been linked to a variety of diseases, including tumorigenesis and immune disorders.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V67588 | A 83-01 sodium | 2828431-89-4 | A 83-01 sodium is a potent inhibitor of TGF-β type I receptors ALK5, ALK4 and ALK7. |
|
V7118 | A77-01 | 607737-87-1 | A 77-01 is a potent inhibitor of the TGF-β type I receptor family ALK5 with IC50 of 25 nM. |
|
V7153 | A83-01 | 909910-43-6 | A-83-01 is an ALK inhibibitor. |
|
V85086 | ALK-5-IN-1 | 1018953-58-6 | |
|
V51372 | ALK2-IN-4 | 2248154-85-8 | ALK2-IN-4 is an effective ALK2 inhibitor. |
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V51373 | ALK2-IN-4 succinate | 2416307-25-8 | ALK2-IN-4 succinate is an effective ALK2 inhibitor. |
|
V83494 | ALK5-IN-10 | 1352608-94-6 | |
|
V88165 | ALK5-IN-80 | ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with IC50 of 3.7 nM. | |
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V67589 | AZ12601011 | 2748337-86-0 | AZ12601011 is an orally bioactive, selective TGFBR1 kinase inhibitor (antagonist) with IC50 of 18 nM and a Kd of 2.9 nM. |
|
V3313 | BIBF0775 | 334951-90-5 | BIBF0775, a 6-substituted indolinone analog, is a novel, potent and selective inhibitor oftransforming growth factor β (TGFβ) type I receptor (Alk5)with anIC50of 34 nM. |
|
V67574 | Bintrafusp alfa (M7824; MSB0011359C) | 1918149-01-5 | Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein consisting of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. |
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V12686 | BIO-013077-01 | 746667-48-1 | BIO-013077-01 is a pyrazole-based TGF-β inhibitor. |
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V80273 | BMPR2-IN-1 | MPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor (antagonist) with IC50 of 506 nM and a KD of 83.5 nM. | |
|
V88159 | BMPR2-IN-1 TFA | BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with IC50 of 506 nM and KD of 83.5 nM. | |
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V88160 | CDD-1653 | 3034216-44-6 | CDD-1653 is a potent and selective BMPR2 inhibitor (IC50=2.8 nM). |
|
V86126 | CREBtide TFA | ||
|
V51269 | Dalutrafusp alfa (AGEN-1423; GS-1423) | 2419918-89-9 | Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific anti-CD73 and TGF-β bifunctional antibody that participates in immunosuppressive pathways. |
|
V94825 | HYL001 | 2426547-83-1 | HYL001 (compound 338) is a potent TGFβ receptor 1 (ALK5) inhibitor that is approximately 9-fold more potent than the structurally related compound galunisertib and is able to eliminate established liver metastases in mice. |
|
V67573 | Isosaponarin | 19416-87-6 | Isosaponarin is a flavonoid glycoside extracted from mustard leaves that can increase collagen synthesis, which is caused by up-regulation of TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase ( Caused by the production of P4H) protein. |
|
V84595 | Itacnosertib (hydrocholide) (TP-0184 (hydrocholide)) | 2409543-84-4 |
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