RSTK
Transforming growth factor-β (TGF-β) family, including TGF-β, activin, Nodal, bone morphogenetic proteins (BMPs) and others, play vital roles in diverse cellular processes, including cell proliferation, differentiation, apoptosis, cell plasticity and migration. The type I receptor serine/threonine kinases (RSTKs) are also known as activin receptor-like kinases (ALKs) for which a systematic nomenclature has been proposed (ALK1-7) Its dysfunctions can result in various kinds of diseases, such as cancer and tissue fibrosis. Ligand binding leads to formation of the receptor heterocomplex, in which TGF-βRII phosphorylates threonine and serine residues of TGF-βRI and thus activates TGF-βRI. The activated TGF-βRI recruits and phosphorylates a subset of SMAD proteins (SMAD 2/3) which are then translocated to the nucleus where they form transcription complexes with DNA binding factors and co-activators/co-repressors to regulate transcription of the target genes[1]. In normal cells, TGF-β, acting through its signaling pathway, stops the cell cycle at the G1 stage to stop proliferation, induce differentiation, or promote apoptosis. When a cell is transformed into a cancer cell, parts of the TGF-β signaling pathway are mutated, and TGF-β no longer controls the cell. These cancer cells proliferate[2].
Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include type I and type II receptors, and transduce signals through Smad-dependent and independent mechanisms. Type I receptors are essential for signaling; and type II receptors are required for binding ligands and for expression of type I receptors. Type I and II receptors form a stable complex after ligand binding, resulting in phosphorylation of type I receptors by type II receptors. Type II receptors are considered to be constitutively active kinases[3],[4].
RSTKs listed: BMP-ALK, TGF-βR
[1] Regulation of TGF-β receptor activity. F. Huang Y.G. Chen. Cell Biosc. 2012, 2-9.
[2] Mechanisms of TGF-beta signaling from cell membrane to the nucleus. Shi Y, Massagué J. Cell. 2003, 113, 685-700.
[3] Activin receptor signaling: a potential therapeutic target for osteoporosis. S. Lotinun, R.S.Pearsall, W.C. Horne, R. Baron Curr. Mol. Pharmacol. 2012, 5, 195-204.
[4] Activin receptor antagonists for cancer-related anemia and bone disease. S.Z. Fields et al. Exp. Opinion Invest. Drugs 2013, 22, 87-101.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2467 | (+)-ITD-1 | Selective inhibitor of TGFβ/Smad signaling that promotes cardiogenesis | €165.00 | |
| 1744 | A 77-01 | TGF-βR 1 inhibitor; ALK 5 inhibitor | €80.00 | |
| 1421 | A 83-01 | TGF-βR 1 inhibitor; ALK 5 inhibitor | €70.00 | |
| 4168 | BMS-986260 | Potent, selective and orally bioavailable TGF-βR 1 inhibitor | €120.00 | |
| 3914 | CDD-1653 | First-in-class, highly potent, and selective BMPR2 kinase inhibitor | €110.00 | |
| 1708 | Dorsomorphin | Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6 | €65.00 | |
| 2150 | Dorsomorphin dihydrochloride | Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6 | €65.00 | |
| 1832 | GW 788388 | TGF-βR 1 inhibitor | €50.00 | |
| 2236 | IN 1130 | TGF-βR 1 inhibitor | €95.00 | |
| 2323 | ITD 1 | Selective inhibitor of TGFβ/Smad signaling that promotes cardiogenesis | €105.00 | |
| 2189 | K 02288 | Inhibitor of BMP signaling. Inhibits ALK1, 2, and 6 | €90.00 | |
| 1509 | LDN 193189 hydrochloride | Highly potent small molecule inhibitor of BMP type I receptors ALK2, ALK3, and ALK6 | €65.00 | |
| 3552 | LDN 212854 | Potent ALK2-biased BMP type I receptor kinase inhibitor | €110.00 | |
| 2201 | LDN 212854 trihydrochloride | Potent ALK2-biased BMP type I receptor kinase inhibitor | €110.00 | |
| 1491 | LY 2157299 | TGF-βR2 inhibitor | €60.00 | |
| 3892 | LY-3200882 | TGF-βR 1 inhibitor | Inquire | |
| 3404 | LY-364947 | Potent, selective and ATP-competitive TGF-βR 1 inhibitor | €90.00 | |
| 1661 | SB 431542 | TGF-βR1 inhibitor; ALK inhibitor | €70.00 | |
| 2197 | SB 505124 | Selective inhibitor of TGF-β type I receptors ALK4 and ALK5 | €95.00 | |
| 2285 | SB 525334 | Potent and selective inhibitor of the TGF-βR1 (ALK5) receptor | €105.00 | |
| 4165 | SB4 | Potent BMP agonist | €80.00 | |
| 1387 | SD 208 | TGF-βR 1 inhibitor | €50.00 | |
| 2903 | SJ000291942 | Activator of the canonical BMP signaling pathway | €95.00 | |
| 2943 | SRI-011381 hydrochloride | TGF-β signaling agonist | €125.00 | |
| 5004 | Stem Cell LSB inhibitor Set | Set of BMP inhibitor LDN 193189 (Axon 1509) and TGF-β inhibitor SB 431542 (Axon 1661) | €90.00 | |
| 5005 | Stem Cell LSC inhibitor Set | Set of LDN 193189 HCl, SB 431542 and CHIR99021, inhibitors of BMP, TGF-β, and GSK-3 resp. | €130.00 | |
| 3076 | TJ191 | Potent and selective anti-cancer agent targeting low TβRIII-expressing malignant T-cell leukemia/lymphoma cells | €120.00 | |