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-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-12071
    LDN193189
    		Inhibitor 99.48%
    LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
  • HY-12071A
    LDN193189 Tetrahydrochloride
    		Inhibitor 99.86%
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-15897
    LDN-212854
    		Inhibitor 99.70%
    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-167864
    M4K2308
    		Inhibitor
    M4K2308 is a selective ether-linked inhibitor of ALK2 with an IC50 of 2 nM. M4K2308 exhibits exceptional selectivity for ALK2 over ALK5 (IC50 of 224 nM). M4K2308 has the potential for the study of diffuse intrinsic pontine glioma (DIPG) research.
  • 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-19628
    OD36
    		Inhibitor 98.70%
    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 98.07%
    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 both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871.
  • HY-145608
    Zilurgisertib
    		Inhibitor 99.77%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK 2 inhibitor for researching diseases such as cancer.
  • HY-112815
    ALK2-IN-2
    		Inhibitor 99.56%
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  • HY-136773A
    KER047 succinate
    		Inhibitor 98.93%
    ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
  • HY-136773
    KER047
    		Inhibitor 99.35%
    ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
  • HY-161376
    M4K2281
    		Inhibitor
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h.
  • HY-151283
    ALK5-IN-33
    		Inhibitor
    ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC50 ≤10 nM.
  • HY-151270
    ALK5-IN-25
    		Inhibitor
    ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC50 ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.
  • HY-148246
    MU1700
    		Inhibitor
    MU1700 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.
  • HY-151273
    ALK5-IN-27
    		Inhibitor
    ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC50 ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).
  • HY-19628A
    OD36 hydrochloride
    		Inhibitor
    OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM.
Cat. No. Product Name / Synonyms Species Source