TGF-β

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].


[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.

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Axon ID Name Description From price
3277 NSC194598 p53 DNA-binding inhibitor €130.00
2501 Pexidartinib Mutil-targeted RTK inhibitor of CSF1R, c-Kit, and FLT3 €80.00
2600 PF 06463922 Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor €105.00
2647 Pirfenidone Broad-spectrum anti-inflammatory and anti-fibrosis agent €60.00
2229 RKI 1447 Potent inhibitor of the Rho-associated ROCK kinases €105.00
2544 S3QEL 2 Suppressor of superoxide production from mitochondrial complex III €60.00
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
1387 SD 208 TGF-βR 1 inhibitor €60.00
2764 SIS3 Potent and selective inhibitor of Smad3 and TGF-βR1 signaling €135.00
2903 SJ000291942 Activator of the canonical BMP signaling pathway €95.00
2943 SRI-011381 hydrochloride TGF-β signaling agonist €125.00
5009 Stem Cell 4i inhibitor Set Set of Thiazovivin, SB 431542, PD 0325901, and CHIR 99021 (inhibitors of ROCK, TGF-β, MEK, and GSK-3 resp.) €170.00
5007 Stem Cell 5i inhibitor Set Set of five inhibitors for neural differentiation of human pluripotent stem cells. €200.00

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