ALK6 Inhibitor

Dorsomorphin (BML-275) is a selective and ATP-competitive AMPK inhibitor (K_i=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).

Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a K_i of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).

Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2^R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC₅₀s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively.

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC₅₀ of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.

CDD-2789 is a potent and selective ALK2 inhibitor with an IC₅₀ 0.54 μM and a K_d of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research.

HM-279 is a potent and orally active ALK5 inhibitor with an IC₅₀ of 4.7 nM. HM-279 shows cross-reactivity with ALK7 (IC₅₀ = 6.8 nM), but HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5-693-fold selectivity. HM-279 demonstrates antitumor activity in vivo through CD8⁺ T cell immunity. HM-279 can be used for the research of colon cancer.

MU1700, a chemical probe, is an orally active and potent ALK1/2 inhibitor with IC₅₀s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.