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
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
2389 AICAR Potent AMPK activator and inducer of differentiation of NSCs €45.00
2187 AS 1892802 Potent, selective, ATP-competitive ROCK inhibitor €95.00
2005 ASP 3026 Inhibitor of the oncogenic fusion kinase EML4-ALK €80.00
5051 Axon Ligands™ Cell signaling and Oncology compound library Axon Ligands™ Cell signaling and Oncology compound library Inquire
5053 Axon Ligands™ Stem cell compound library Axon Ligands™ Stem cell compound library Inquire
2153 AZD 3463 Potent inhibitor of ALK and IGF1R €105.00
2978 Brigatinib Potent, selective, and orally active anaplastic lymphoma kinase (ALK) inhibitor €80.00
2753 CCG 232601 Rho/MRTF/SRF transcriptional pathway inhibitor €160.00
3092 CCG-203971 Rho/MRTF/SRF transcriptional pathway inhibitor €60.00
3069 CCG-222740 Potent and selective Rho/MRTF/SRF transcriptional pathway inhibitor €145.00
1884 CH 5424802 Orally available and selective ALK inhibitor €80.00
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
1167 GSK 269962A ROCK1 and ROCK2 inhibitor €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
2780 KD025 Selective ATP-competitive inhibitor of ROCK2 €95.00
2294 KRCA 0008 Potent and selective dual ALK/ACK1 inhibitor with good drug-like properties €95.00
2395 KY 05009 Inhibitor of TNIK that attenuates TGF-β1-mediated Wnt and Smad signaling €125.00
2224 LDK 378 Potent, bioavailable, and selective anaplastic lymphoma kinase (ALK) inhibitor €95.00
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
3404 LY-364947 Potent, selective and ATP-competitive TGF-βR 1 inhibitor €90.00

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