TGF-β Receptor Inhibitor

Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.

GDF15 Human Pre-designed siRNA Set A contains three designed siRNAs for GDF15 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).

ALK-5-IN-1 is an ALK-5 inhibitor. ALK-5-IN-1 can be used for the research of cancer, and conditions involving fibrosis.

Salviamarinic acid A is a water-soluble phenolic acid that can be extracted from Salvia miltiorrhiza with potent anti-pulmonary fibrosis activity. Salviamarinic acid A significantly increases cell viability, cell index, cell motility and E-cadherin expression, and reduces TGF-β1, α-SMA and Collagen I levels. Salviamarinic acid A can be used for pulmonary fibrosis research.

sGC stimulator 1 is a carbonyl sulfide (COS)/H₂S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC₅₀ = 496 nM). sGC stimulator 1 exhibits a well-characterized H₂S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H₂S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H₂S. sGC stimulator 1 can be used for the study of heart failure (HF).

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.

LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC₅₀ = 0.2 μM) and LIFR inhibitor (IC₅₀ = 7.9 μM). LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF)-mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders.

ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC₅₀ values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.

Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.

Anti-Candida auris β-1,3-glucans Antibody (2G8) is an antibody targeting Candida auris β-1,3-glucans, and also acts as an inhibitor of AChE and TGF-β receptor 2. Anti-Candida auris β-1,3-glucans Antibody (2G8) also targets fungal cell wall components, effectively inhibits fungal growth and interferes with capsule formation, thereby significantly reducing the fungal load in mouse tissues. Anti-Candida auris β-1,3-glucans Antibody (2G8) not only blocks TGF-β receptor binding to inhibit the Smad signaling pathway, reduces fibroblast activation and collagen deposition, but also induces epithelial differentiation of tumor cells and reduces pancreatic tumor metastasis. Anti-Candida auris β-1,3-glucans Antibody (2G8) specifically binds to the conserved N-linked glycoepitope on AChE to inhibit its activity without interfering with BChE, and can be used in studies of cryptococcosis and related tumor mechanisms.The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC₅₀ of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.

Pixofisiran sodium scrambled negative control is the sequence scrambled negative control of Pixofisiran sodium.

Clonixin-¹³C,d₃ (SCH-10304-¹³C,d₃) is the deuterium and ¹³C-labeled Clonixin (HY-121235). Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca²⁺ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.

K02288 (GMP) is K02288 (HY-12278) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC₅₀s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC₅₀s of of 5-34 nM.

GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a K_i of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension.

TGF-βR1/VEGFR2-IN-1 is a dual inhibitor targeting TGF-βR1/VEGFR2, with an IC₅₀ of 232.5 nM against human TGF-βR1 and an IC₅₀ of 371.4 nM against human VEGFR2. TGF-βR1/VEGFR2-IN-1 mediates antiproliferative effects by inhibiting the TGF-βR1 and VEGFR2 signaling pathways. TGF-βR1/VEGFR2-IN-1 can be used in research related to colorectal cancer, non-small cell lung cancer, cervical cancer, and hepatocellular carcinoma.

ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC₅₀ ≤10 nM.

Axl-IN-21 is an orally active and selective AXL inhibitor (K_d = 2.7 nM, IC₅₀ = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with K_d = 1.4 nM, DDR1 with IC₅₀ = 22.2 nM, HIPK4 with K_d = 11.0 nM and LOK with K_d =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer^{[1] [2]} .

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