TNF Receptor Inhibitor

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signaling pathways. Akt/NF-κB/JNK-IN-1 inhibits nitric oxide production with an IC₅₀ of 3.15 μM. Akt/NF-κB/JNK-IN-1 shows anti-inflammatory activities.

1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models.

S101 is an inhibitor of SLP-76 and AhR. By inhibiting SLP-76 phosphorylation, S101 blocks the TCR signaling pathway and prevents AhR nuclear translocation, thereby selectively suppressing the proliferation of activated T cells, inducing their apoptosis, and reducing TNF-α levels. S101 can be used in studies of graft rejection, psoriasis, and superantigen-induced toxic shock.

Trigraecum is a flavonoid compound found in Dracaena steudneri and Dalbergia cochinchinensis, exhibiting anti-inflammatory activity. It can inhibit the LPS (HY-D1056)-induced production of IL-1β, IL-2, GM-CSF, and TNF-α in human peripheral blood mononuclear cells. Trigraecum holds promise for research on inflammatory diseases.

Gaultherin (Standard) is the analytical standard for Gaultherin (HY-N1965). Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC₅₀ = 0.35 mg/mL), LOX (IC₅₀ = 0.56 mg/mL) and HYAL (IC₅₀ = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).

Pexmetinib (Standard) (ARRY-614 (Standard)) is the analytical standard of Pexmetinib (HY-16782). This product is intended for research and analytical applications. Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

D-chiro-Inositol is a stereoisomer of inositol that exhibits activities such as improving glucose metabolism, anti-tumor effects, anti-inflammatory properties, and antioxidant activity. D-chiro-Inositol effectively alleviates cholestasis by enhancing bile acid secretion and reducing oxidative stress. D-chiro-Inositol improves insulin resistance, lowers hyperglycemia and circulating insulin levels, reduces serum androgen levels, and ameliorates some metabolic abnormalities associated with X syndrome by mimicking the action of insulin. Additionally, D-chiro-Inositol can induce a reduction in pro-inflammatory factors (such as Nf-κB) and cytokines (such as TNF-α), thereby exerting anti-inflammatory effects. D-chiro-Inositol may be used in the study of liver cirrhosis, breast cancer, type 2 diabetes, and polycystic ovary syndrome.

BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.

13 (S)-HOTrE is an oxylipin metabolite of α-Linolenic acid (HY-N0728). 13 (S)-HOTrE mediates the inactivation of the NLRP3 inflammasome through the PPAR-γ pathway to exert anti-inflammatory effects. 13 (S)-HOTrE inhibits NF-κB nuclear translocation, ROS production, autophagy and IL-1β levels, induces apoptosis, and increases IL-10 levels. 13 (S)-HOTrE alleviates LPS-induced inflammatory responses in macrophages, prolongs the survival time of septic mice, and regulates the immunometabolic phenotype in parenteral nutrition mouse models. 13 (S)-HOTrE can be used in the research of immune and inflammation-related diseases.

Naphazoline (nitrate) (Standard) is the analytical standard of Naphazoline (nitrate). This product is intended for research and analytical applications. Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline nitrate can be used for non-bacterial conjunctivitis research.

Betamethasone succinate (NSSL-BMS) is a nano-formulation that can cross the blood-brain barrier. Betamethasone succinate is prepared by encapsulating the Betamethasone (HY-13570) semi-succinate in PEG-liposomes. Betamethasone succinate utilizes the enhanced permeation and retention effects of liposomes to target and deliver the potent glucocorticoid to the inflammatory sites. Betamethasone succinate inhibits the secretion of pro-inflammatory cytokines (such as TNF-α and IL-6) while maintaining the level of anti-inflammatory cytokine TGF-β. Betamethasone succinate can be used in the research of arthritis and cerebral malaria.

2'-Acetylacteoside (Standard) is the analytical standard of 2'-Acetylacteoside (2'-AA) (HY-N0026). This product is intended for research and analytical applications. 2'-Acetylacteoside is a natural compound with oral activity and blood-brain barrier permeability. 2'-Acetylacteosideexhibits MAO‑B inhibitory activity (IC₅₀ = 17.71 μM, K_i = 13.81 μM). 2'-Acetylacteoside downregulates the expression of RANK, TRAF6, NF‑κB, NFATc1 and IKKβ, disrupts the RANKL/RANK interaction, blocks downstream signaling pathways, and increases the level of phosphorylated Akt. 2'-Acetylacteoside possesses potent anti-osteoclastogenic, anti-bone resorptive, pro-neurogenic, neuroprotective and antioxidant activities. 2'-Acetylacteoside can be used in the research of osteoporosis, ischemic stroke and Parkinson's disease.

Isoforskolin (Standard) is the analytical standard of Isoforskolin. This product is intended for research and analytical applications. Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.

Bruceoside B is a PI3K/Akt/NF-κB inhibitor. Bruceoside B reduces LPS (HY-D1056)-induced nitric oxide release and the secretion of TNF-α, IL-6 and IL-1β, and decreases the activation level of apoptosis. Bruceoside B inhibits the replication, coat protein accumulation and local lesion formation of tobacco mosaic virus (TMV), and enhances the anti-infection ability of plants. Bruceoside B can be used in studies related to acute lung injury and tobacco mosaic virus infection.

CD28-IN-4 is a selective CD28 inhibitor with a human IC₅₀ of 231 nM and a human K_d of 344 nM. CD28-IN-4 binds to CD28, disrupts its interaction with CD80, blocks CD28-mediated co-stimulatory signal transduction, and reduces cytokine secretion in a human primary tumor-PBMC and epithelial tissue co-culture model. CD28-IN-4 can be used for cancer-related research.

CD28-IN-3 is a CD28 inhibitor with an IC₅₀ of 7.80 μM and a Kd of 52.45 μM. CD28-IN-3 selectively blocks the CD28-B7 interaction, thereby inhibiting CD28-mediated costimulation. CD28-IN-3 suppresses the production of proinflammatory cytokines IFN-γ, IL-2 and TNF-α. CD28-IN-3 can be used in the research of checkpoint-resistant cancers.

Taurohyodeoxycholic acid-d4 (sodium) is a deuterated labeled Taurohyodeoxycholic acid (sodium). Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.

Talmapimod (Standard) is the analytical standard of Talmapimod (HY-10406). This product is intended for research and analytical applications. Talmapimod (SCIO-469) is an orally active and selective inhibitor of p38α MAPK with an IC₅₀ of 9 nM. Talmapimod inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. Talmapimod inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).

Ecliptasaponin A (Standard) is the analytical standard for Ecliptasaponin A (HY-N1508). Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.

Xanthine oxidase-IN-21, a Genipin (HY-17389) derivative, is an orally active mixed competitive xanthine oxidase (XOD) inhibitor with an IC₅₀ of 0.68 μM. Xanthine oxidase-IN-21 reduces renal fibrosis by decreasing α-SMA expression and suppresses pro-inflammatory cytokines IL-1β, IL-6, and TNF-α through NF-κB pathway regulation. Xanthine oxidase-IN-21 also inhibits URAT1 and GLUT9 expression, promoting uric acid excretion and lowering serum uric acid levels. Xanthine oxidase-IN-21 shows significantly hepatorenal protection activity. Xanthine oxidase-IN-21 can be used for the research of hyperuricemia.