2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor
  5. ALK2 Isoform

ALK2

Activin A receptor type 1 (ACVR1), also known as ALK2, is a bone fide BMP receptor. Various TGFβ, Activin, and BMP ligands, such as BMP9 and Activin B, have been found to induce ALK2 signaling. In Leydig cells, which are found in the testes, ALK2 can inhibit Activin signaling by blocking Activin A access to the type II receptor by forming a type II/type I receptor complex in the absence of ligand. When it acts in this manner, ALK2 has an inhibitory function. Interestingly, induction of signaling through non-TGFβ family ligands has been noted. For example, it was found that stress-induced phosphoprotein 1 (STIP1) can bind directly to ALK2, independent of a type II receptor, to induce downstream Smad signaling. Primarily studied for its role in osteogenesis and chondrogenesis, ALK2 is required for chondrocyte proliferation and differentiation.

Cat. No. Product Name Effect Purity
  • HY-13418A
    Dorsomorphin
    		Inhibitor 99.91%
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=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).
  • HY-12071
    LDN193189
    		Inhibitor 99.72%
    LDN193189 (DM-3189) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
  • HY-13418
    Dorsomorphin dihydrochloride
    		Inhibitor 99.91%
    Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki 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).
  • HY-12071A
    LDN193189 Tetrahydrochloride
    		Inhibitor 99.79%
    LDN193189 (DM-3189) Tetrahydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
  • 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-149591
    M4K-2009
    		Inhibitor 99.35%
    M4K-2009 is an orally bioactive ALK2 inhibitor with an IC50 of 13 nM. M4K-2009 exerts comparable inhibitory potency against wild-type and mutant ALK2G328V, ALK2R206H, and ALK2R258G. M4K-2009 exhibits moderate off-target inhibitory activity against hERG potassium channels. M4K-2009 can be used in studies related to diffuse intrinsic pontine glioma.
  • HY-P991855
    RKER-216
    		Inhibitor
    RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation.
  • 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-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-145608
    Zilurgisertib
    		Inhibitor 98.25%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK2 inhibitor with an IC50 value of 15 nM. Zilurgisertib inhibits SMAD1/5 phosphorylation with an IC50 value of 63 nM. Zilurgisertib inhibits hepcidin production and improve anemia. Zilurgisertib can be used in melanoma research.
  • HY-19628
    OD36
    		Inhibitor 99.33%
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
  • 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-109179
    Itacnosertib
    		Inhibitor 99.06%
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity.
  • HY-112815
    ALK2-IN-2
    		Inhibitor 99.93%
    ALK2-IN-2 is an orally active and selective inhibitor of ALK2 (ACVR1), with an IC50 value of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 can inhibit oxidative stress and protect endothelial cells.
  • HY-136773
    KER047
    		Inhibitor 98.80%
    KER047 (ALK2-IN-4) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
  • HY-109179A
    Itacnosertib hydrochloride
    		Inhibitor 99.43%
    Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.
  • HY-136773A
    KER047 succinate
    		Inhibitor 98.93%
    KER047 succinate (ALK2-IN-4 succinate) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 succinate can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
  • 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.
Cat. No. Product Name / Synonyms Species Source