TGF-β Receptor Inhibitor

TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research.

SAR-439459 is a human monoclonal antibody (mAb) targeting TGFB1/TGFβ-1. SAR-439459 blocks TGFβ-mediated pSMAD signaling, and suppression of T cells and NK cells. SAR-439459 has anti-tumor activity .

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 K_Ds of 37 nM.

Nadecnemab is an IgG4κ antibody targeting to GFRA3, glial cell derived neurotrophic factor family receptor alpha 3. Nadecnemab can be used for research of osteoarthritis of the knee/pain.

Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific bifunctional antibody against CD73 and TGF-β, which is involved in the immunosuppressive pathway.

Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).

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

KY1070 is a fully human anti-BMP6 antibody with a K_d of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease ^{[1] [2]}.

TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC₅₀ values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .

TGFβR-IN-1 is a long-acting tumor-activated proagent of a TGFβR inhibitor.

Dexamethasone sodium phosphate solution is mainly composed of Dexamethasone phosphate disodium (HY-B1829A). Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).

Cilengitide (Standard) (EMD 121974 (Standard)) is the analytical standard of Cilengitide (HY-16141). This product is intended for research and analytical applications. Cilengitide (EMD 121974) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

Galunisertib monohydrate is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC₅₀ of 56 nM.

Tgfbr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tgfbr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Omtriptolide sodium (PG490-88Na) is a derivative of Triptolide (HY-32735). Omtriptolide sodium exhibits significant immunosuppressive, anti-fibrotic and anti-inflammatory properties. The mechanism of action of Omtriptolide sodium is diverse, including inhibiting T cell activation and proliferation, inducing T cell apoptosis (apoptosis), blocking fibroblast maturation/proliferation, inhibiting TGF-β mRNA expression, and suppressing pro-inflammatory cytokines (such as IL-2, IFN-γ, TNF-α) by blocking transcription factors such as NF-κB. Omtriptolide sodium can be used for research on obstructive airway diseases, pulmonary fibrosis and graft-versus-host disease.

TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma.

TGFβRI-IN-6 (compound 22) is a potent TGFβRI inhibitor with an IC₅₀ value of 0.55 nM. TGFβRI-IN-6 has the potential to enhance anti-tumor immunity.

ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC₅₀s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer.

TGFBR1 Human Pre-designed siRNA Set A contains three designed siRNAs for TGFBR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

VPI-2690B is a human monoclonal antibody (mAb) targeting Integrin aVb3. VPI-2690B inhibits TGF-β signaling. VPI-2690B can be used in Diabetic nephropathies research.