TGF-β Receptor Inhibitor

ALK2-IN-7 is a ALK2 (ACVR1) inhibitor. ALK2-IN-7 is applicable to studies related to BMP/ALK2 signaling, anemia associated with iron homeostasis imbalance, and multiple osteochondromas.

M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC₅₀ of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6.

Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC₅₀ = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis.

ALK2-IN-6 (Compound 14a) is a selective ALK2 inhibitor, with an IC₅₀ of 9 nM. ALK2-IN-6 can be used in the research of diffuse intrinsic pontine glioma.

PF-06940434 (ADWA-11) is a monoclonal antibody targeting integrin αvβ8. PF-06940434 inhibits αvβ8-mediated TGF-β activation. PF-06940434 increases the accumulation of tumor-infiltrating CD8⁺ T cells and upregulates the expression of granzyme B and TNF-γ. PF-06940434 blocks the inhibitory effect of CD4⁺CD25⁺ T cells on the cytotoxic activity of tumor CD8⁺ T cells. PF-06940434 enhances the anti-tumor efficacy of combination therapies with other immunomodulators or radiotherapy and induces long-term anti-tumor immunity. PF-06940434 can be used in the research of squamous cell carcinoma, breast cancer, colon cancer, and prostate adenocarcinoma.

TJN-331 is a potent and orally active TGF-β1 Inhibitor. TJN-331 ameliorates anti-glomerular basement membrane (GBM) nephritis in rats by inhibitng TGF-β1 production, thereby reducing extracapillary proliferation in glomeruli. TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. TJN-331 can be used for the research of nephritis and IgA nephropathy.

ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).

TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC₅₀s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.

TP0427736 is a selective inhibitor of ALK5 with an IC₅₀ of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells.

DMH-1 (GMP) is GMP grade DMH-1 (HY-12273). DMH-1 (GMP) is a selective BMP inhibitor. DMH-1 (GMP) upregulates the expression of SOX1. DMH-1 (GMP) increases cardiomyocyte progenitor cells and promotes the differentiation of mouse embryonic stem cells into cardiomyocytes. DMH-1 (GMP) induces the differentiation of hiPSC-derived neural progenitor cells into β3-tubulin-positive neurons.

RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.

Vactosertib (Standard) is the analytical standard of Vactosertib (HY-19928). This product is intended for research and analytical applications. Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like K_inase 5 (ALK5) inhibitor with an IC₅₀ of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC₅₀ of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.

CDD-1281 is a highly potent and selective BMPR2 kinase inhibitor with an IC₅₀ of 1.2 nM. CDD-1281 can effectively inhibit BMP-mediated gene expression.

LY2109761 (Standard) is the analytical standard of LY2109761. This product is intended for research and analytical applications. LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.

Gdf15 Rat Pre-designed siRNA Set A contains three designed siRNAs for Gdf15 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC₅₀ value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis.

NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice.

LDN193189 (DM-3189) dihydrochloride (Standard) is the analytical standard of LDN193189 dihydrochloride (HY-12071B). This product is intended for research and analytical applications. LDN193189 (DM-3189) dihydrochloride 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.

SD-208 (Standard) is the analytical standard of SD-208. This product is intended for research and analytical applications. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.