TGF-β Receptor Inhibitor

TP-DEA2, a predictable-release Triptolide (HY-32735) prodrug, block Bleomycin-induced pulmonary fibrosis and inflammation. TP-DEA2 significantly inhibits α-SMA production.

ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with an IC₅₀ value of 3.7 nM. ALK5-IN-80 can be used for cancer research.

RO-7303509 (MTBT1466A; RG-6315) is a human monoclonal antibody and TGFβ3 neutralizer. RO-7303509 targets the profibrotic mediator TGFβ3 to alleviate fibrosis. RO-7303509 can be administered via subcutaneous or intravenous routes and is used in research on systemic sclerosis. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).

Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a K_i value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions.

J-1149 is a potent ALK5 inhibitor, with an IC₅₀ value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC₅₀ value of 0.435 μM. J-1149 can be used for liver fibrosis research.

ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC₅₀≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.

TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC₅₀ of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference agent against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.

TGFβ1-IN-2 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-2 can be used for idiopathic pulmonary fibrosis (IPF) research.

TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research.

RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a K_D 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.

Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

LY2382770 is a human monoclonal antibody (mAb) targeting TGFB1. LY2382770 can be used in dabetic nephropathies research.

TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC₅₀ values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 %.

ALK5-IN-7 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-7 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 4).

ActRIIB-IN-3 is a ActRIIB inhibitor. ActRIIB-IN-3 inhibits the ActRIIB protein in the MSTN pathway and induces the reversal of skeletal muscle atrophy associated with cancer cachexia. ActRIIB-IN-3 is applicable for the research of cancer cachexia.

CDD-1115 is a BMPR2 serine/threonine kinase inhibitor with an IC₅₀ of 1.8 nM against human BMPR2 kinase. CDD-1115 selectively inhibits the catalytic activity of BMPR2, and shows weak inhibitory effects on ALK1 and ALK2.

CDD-1431 is a low-nanomolar selective kinase inhibitors of BMPR2, with K_iapp value of 20.6 nM. CDD-1431 suppresses BRE-reporter activity, with an IC₅₀ of 4.87 μM. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation.

ActRIIB-IN-2 is an ActRIIB inhibitor with an IC₅₀ of 1.1 nM. ActRIIB-IN-2 can be used for the research of cancer cachexia.

TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC₅₀ of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network.

7-O-Galloyl-D-sedoheptulose is an orally effective polyphenolic compound. 7-O-Galloyl-D-sedoheptulose lowers the serum levels of glucose, leptin, insulin, C-peptide, resistin, TNF-α, IL-6, and increases the serum level of adiponectin. 7-O-Galloyl-D-sedoheptulose significantly reduces the levels of ROS and lipid peroxidation products (TBARS) by down-regulating the protein expression of NADPH oxidase subunit Nox-4 and p22phox. 7-O-Galloyl-D-sedoheptulose down-regulates NF-κB and related pro-inflammatory factors (COX-2, iNOS), inhibits the phosphorylation of JNK and the activity of its downstream AP-1. 7-O-Galloyl-D-sedoheptulose reduces the expression of TGF-β1 and fibronectin, indicating its potential in anti-tissue fibrosis. 7-O-Galloyl-D-sedoheptulose can be used for the study of type 2 diabetes and its hepatic and pancreatic complications.