tgfβri

TGFβRI-IN-1 is an orally active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively.

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively).

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. It effectively inhibits the phosphorylation of SMAD2/3 and reduces the viability of H22 cells, with IC50 values of 12 nM and 65 nM, respectively. In an H22 cell xenograft model, TGFβRI-IN-7 exhibits antitumor efficacy with a TGI of 79.6%.

TGFβRI-IN-5 (Compound 4b) is a potent TGFβRI inhibitor with an IC50 of 0.08 μM, demonstrating significant anticancer activity by enhancing apoptosis and arresting the G2/M phase of the cell cycle in all tested cell lines[1].

TGFβRI-IN-4 is a potent, orally active TGFβ receptor type I kinase (TGFβRI) inhibitor that targets ALK5 (IC50: 44 nM) and NIH3T3 (IC50: 42.5 nM), inhibiting tumor growth and weight in a xenograft tumor model.

TGFβRI-IN-6 is a potent TGFβRI inhibitor with an IC50 value of 0.55 nM.TGFβRI-IN-6 has the potential to enhance anti-tumour immunity.

TGF-βRI inhibitor 3 (Compound 9ac) is a selective inhibitor of TGF-β that effectively suppresses the TGF-β signaling pathway. It exhibits IC50 values of 13 μM for c-Src kinase and 0.63 μM for ALK5 kinase.

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) with an IC50 of 4.1 μM. It inhibits TGFβ signaling by promoting protein degradation of TGFβ RII. Additionally, TGFβRI-IN-7 can block the transition from endothelial to mesenchymal states and inhibit cell migration, making it useful for cancer research.

TGFβRII-IN-2 (Compound 3n) acts as an inhibitor of TGFβRII with an IC50 of 2.4 μM. It effectively blocks the transition from epithelial to mesenchymal states and inhibits cell migration in various cancer cell lines without disrupting the microtubule network.

RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.

ALK5-IN-10 is a potent ALK5 inhibitor with an IC50 of 7nM.

LDN 193688 is a BMP kinase inhibitor preferential for the ALK2 site, acting by binding to the ALK site, with BMP inhibitory activity 100 times that of TGFβRI, used in the study of progressive osseous fibrodysplasia.

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor (KD: 0.01 μM) and antimicrobial agent. It serves as a substrate for cytochrome P450. The compound contains a pyridyl-6-methyl group, essential for inhibiting Mycobacterium tuberculosis, and effectively inhibits non-replicating and persistent strains of this bacterium.

Ontunisertib (Example 26) is a TGFβ receptor I/ALK5 (TGFβRI/ALK5) inhibitor with an IC50 value range of 100-500 nM for TGFβRI and an IC50 value of ≤100 nM for ALK5. This compound is applicable for research in gastrointestinal diseases, fibrosis-related conditions of the skin and eyes, and cancer.

SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).

(E/Z)-BIX 02189 is an isomer of BIX 02189 that can be employed in biochemical experiments.

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1].