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-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.

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].

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.

Compound 12d is a potent ALK5 inhibitor with an IC50 of 7nM.

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

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

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.

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.

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).

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.

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

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.

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

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].

ALK5-IN-9 is a potent, orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation (IC50: 25 nM) and inhibits NIH3T3 cell activity (IC50: 74.6 nM). ALK5-IN-9 has shown research potential in cancer diseases.