2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor
  5. ACVR2A Isoform

ACVR2A

ACVR2A encodes activin receptor type 2A, a TGF-β family type II receptor that binds activin and participates in receptor complexes driving Smad2/3 signaling[1]. Mechanistically, Activin A uses ACVR1B as the type I receptor with ACVR2A or ACVR2B as type II receptors, distinguishing ACVR2A from type I receptors that define downstream pathway output[2]. In gastrointestinal cancer models, ACVR2 coding microsatellites undergo frameshift mutation in mismatch repair-deficient cells, which abrogates TGF-β family receptor signaling[3]. In MSI-high colon cancer, ACVR2 mutation occurred in 83% of tumors and frequently caused loss of ACVR2 protein expression[4]. In colorectal cancer with microsatellite instability, ACVR2 frameshift mutation was reported in 92% of tumors, supporting its use as a molecular feature for MSI-focused tumor biology studies[5]. Compared with related pathway receptors, ACVR2A should therefore be studied with attention to ACVR2B and ACVR1B co-receptor context, ligand-dependent Smad2/3 readouts, and mutation-driven loss-of-function models[2][3][4].

Cat. No. Product Name Effect Purity
  • HY-P99355
    Bimagrumab
    		Inhibitor 99.31%
    Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness.
  • HY-P99590
    Sotatercept
    		99.94%
    Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions.
  • HY-157442
    GLPG3312
    		Antagonist 98.63%
    GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
  • 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-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.
Cat. No. Product Name / Synonyms Species Source