2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor
  5. ALK1 Isoform

ALK1

ALK1 (activin receptor-like kinase 1), encoded by ACVRL1, is an endothelial-enriched transmembrane serine/threonine kinase receptor within the transforming growth factor-β (TGF-β) receptor superfamily that plays a central role in vascular development, endothelial homeostasis, and angiogenic regulation[1][2][3]. Mechanistically, ALK1 functions as a type I receptor that responds primarily to the circulating ligands BMP9 and BMP10, activating downstream SMAD1/5/8-dependent transcriptional programs that regulate endothelial behavior and vascular quiescence[4][5][6]. Continuous BMP10-mediated ALK1 signaling is required for vascular maintenance, and disruption of this pathway leads to arteriovenous malformations, highlighting its importance in endothelial integrity[4]. Consistent with this function, loss-of-function mutations in ACVRL1 are a major cause of hereditary hemorrhagic telangiectasia type 2 (HHT2), a vascular disorder characterized by abnormal artery-vein connections and pathological angiogenesis[1][4][7]. ALK1 mutations have also been associated with pulmonary arterial hypertension and altered endothelial transcriptional responses to BMP9 and BMP10 stimulation. Compared with related TGF-β family type I receptors, ALK1 exhibits marked endothelial-cell specificity, particularly in arterial endothelial cells, distinguishing its biological role from more broadly expressed receptor kinases[1][2]. For experimental applications, recombinant BMP9 and BMP10 are widely used to activate ALK1 signaling, whereas ALK1-targeting antagonists and ligand-trap strategies have been investigated to modulate angiogenesis and vascular remodeling in preclinical disease models, including cancer-associated angiogenesis[6][8][9].

Cat. No. Product Name Effect Purity
  • HY-16712
    LDN-214117
    		Inhibitor 99.54%
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
  • HY-15897
    LDN-212854
    		Inhibitor 99.62%
    LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).
  • HY-12274
    ML347
    		Inhibitor 99.94%
    ML347 (LDN193719) is a highly selective ALK1/ALK2 inhibitor. ML347 has IC50 values of 46 and 32 nM against ALK1 and ALK2, respectively, >300-fold selective over ALK3. ML347 block the phosphorylation of Smad1/5 by TGF-β1.
  • HY-117887
    Fidrisertib
    		Inhibitor 98.17%
    Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively.
  • HY-123900
    AZ12799734
    		Inhibitor 98.67%
    AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.
  • HY-185430
    HM-279
    		Inhibitor
    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.
  • HY-173149
    CDD-2789
    		Inhibitor
    CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd 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.
  • HY-148246
    MU1700
    		Inhibitor
    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.
Cat. No. Product Name / Synonyms Species Source