tgfβr1

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.

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.

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

BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

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].

TGFβ-IN-3 (Compound 8) is a long-acting prodrug that acts as a TGFβR1 inhibitor with tumor-targeting activation. It enables selective drug release within tumors, offering a 2.2-fold increase in the tumor-to-blood ratio. TGFβ-IN-3 is applicable for colon cancer research.

TP-0427736 is a novel potent and selective ALK5 inhibitor (IC50: 2.72 nM). P0427736 was 300-fold higher than the inhibitory effect on ALK3. TP0427736 reduces TGF-β induced growth inhibition in human outer root sheath cells and elongates the anagen phase i

EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.

BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).