Catalog No.
Product Name
Application
Product Information
Citations
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TLR4/MyD88/NF-κB Inhibitor
SjDX5-271 is a small peptide inhibitor targeting the TLR4/MyD88/NF-κB signaling pathway. It is known to induce cell polarization and mitigate hepatic inflammation, demonstrating protective effects against liver ischemia-reperfusion injury in mouse models. This compound is valuable for research in immunology and liver-related inflammation studies. -
Anti-Inflammatory Agent
4-Methoxylonchocarpin is an orally active anti-inflammatory agent that primarily targets Toll-like Receptor 4 (TLR4). This compound effectively inhibits the binding of lipopolysaccharides (LPS) to TLR4, leading to the suppression of NF-κB activation and the downregulation of pro-inflammatory cytokines such as TNF and IL-6. Additionally, 4-Methoxylonchocarpin reduces the phosphorylation of TGF-beta activated kinase 1 and mitigates the expression of IL-1β, IL-17A, and TNF in a 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model, demonstrating its potential in anti-inflammatory research applications. -
Anti-inflammatory Agent
Chlojaponilactone B is a lindenane-type sesquiterpenoid known for its anti-inflammatory properties. This compound functions by inhibiting Toll-like receptor 4 (TLR4), leading to a decrease in reactive oxygen species (ROS) production and downregulation of the NF-κB pathway. Consequently, it reduces the expression of pro-inflammatory cytokines, including iNOS, nitric oxide (NO), COX-2, IL-6, and TNF-α. Chlojaponilactone B is a valuable tool for research into inflammation and related pathways. -
TLR7/TLR9 Inhibitor
ODN 24888 is a guanine-modified inhibitory oligonucleotide (INH-ODN) that specifically targets TLR7 and TLR9 signaling pathways. It effectively inhibits interferon-alpha (IFN-α) secretion and NF-κB activation, while also reducing interleukin-6 (IL-6) release. ODN 24888 is valuable for studying immune and inflammatory responses and can be utilized as a vaccine adjuvant in various research applications. -
TLR Inhibitor
TIC10g is a dual inhibitor of toll-like receptors 7 and 9 (TLR7 and TLR9). It effectively decreases TNF-α release in mouse macrophages and human B lymphocytes, with IC50 values of 14.5 μM and 6.5 μM for TLR7, and 7.69 μM and 11.5 μM for TLR9, respectively. TIC10g also inhibits the activation of NF-κB and MAPK pathways, demonstrating potential as an anti-inflammatory agent in conditions such as systemic lupus erythematosus and rheumatoid arthritis. -
TLR4 Signaling Inhibitor
NCI126224 is a TLR4 signaling inhibitor that modulates immune responses by suppressing lipopolysaccharide (LPS)-induced production of key inflammatory mediators, including NF-κB, TNF-α, IL-1β, and nitric oxide. This compound demonstrates biological activity in the low nanomolar to low micromolar range, making it a valuable tool for research into inflammatory diseases and their mechanisms. Its ability to interfere with TLR4 signaling pathways positions NCI126224 as a significant reagent for exploring potential therapeutic strategies in inflammation-related studies. -
TLR4/NF-kB/MAPK Inhibitor
TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
TLR1/2 Agonist
SMU-C409 is a Toll-like receptor 1/2 (TLR1/2) agonist, exhibiting an EC50 of 65 nM in HEK-Blue hTLR2 cells. It activates the TLR1/2–MyD88–NF-κB signaling pathway, leading to increased secretion of pro-inflammatory cytokines TNF-α and IL-1β, which promotes robust immune cell activation. With low toxicity observed in vitro, SMU-C409 serves as a valuable tool for cancer immunotherapy research. -
TLR1/2 Heterodimer Agonist
SMU-C68 is a selective small-molecule agonist of the TLR1/2 heterodimer, with an EC50 value of 0.009 μM. It effectively activates the NF-κB and MAPK signaling pathways, leading to the release of pro-inflammatory cytokines such as TNF-α and IL-1β. This compound is a valuable tool for investigating mechanisms of inflammation and cancer biology in research applications. -
NF-κB Inhibitor
NF-κB-IN-14 is an NF-κB inhibitor that effectively modulates inflammatory responses by significantly inhibiting nitric oxide production in LPS-stimulated macrophages, with an IC50 of 6.4 μM. This compound disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway. Additionally, NF-κB-IN-14 has demonstrated efficacy in reducing ear edema and inflammation in a mouse model of atopic dermatitis, highlighting its potential utility in inflammatory research. -
Toll-like Receptor (TLR) Ligand
Ste2Cys is a diacylglycerol cysteine-type lipid molecule that serves as a ligand for Toll-like Receptor 2 (TLR2). It activates the NF-κB signaling pathway, leading to the upregulation of MHC II class molecules on the surface of mouse bone marrow-derived dendritic cells. This compound is valuable for research into the development of immunologic vaccines and enhancing immune responses. -
TLR2 Agonist
TLR2 Agonist 1 is a highly potent agonist for human toll-like receptor 2 (TLR2), exhibiting an EC50 of 116 pM. It activates NF-κB promoter activity through TLR2/TLR1 heterodimerization, making it a valuable tool for studying TLR-mediated immune responses. This compound is applicable in research focused on inflammation, innate immunity, and potential therapeutic strategies involving TLR pathways. -
MyD88 Inhibitor
LM9 is a selective inhibitor of MyD88, a key adaptor protein in the Toll-like receptor (TLR) signaling pathway. By blocking the binding of TLR4 to MyD88, LM9 disrupts MyD88 homodimer formation and subsequent activation of the NF-κB signaling pathway. This compound demonstrates significant anti-inflammatory effects, mitigating atherosclerosis and fibrosis in models of obesity-induced cardiomyopathy. LM9 is valuable for research focused on understanding the mechanisms of inflammation, fibrosis, and cardiovascular diseases. -
μ Opioid Receptor Antagonist
β-Funaltrexamine (β-FNA) is an irreversible and selective antagonist of the μ-opioid receptor. This compound demonstrates significant anti-inflammatory and neuroprotective properties by modulating TLR4 signaling, inhibiting cytokine-induced iNOS activation, and reducing neuroinflammation. Additionally, β-FNA influences NF-κB signaling and chemokine expression in human astrocytes and murine models. It is an important tool for research into neurodegenerative diseases, including stroke. -
Steroidal Alkaloid Glycoside
Esculeoside A is a spirosolane-type steroidal alkaloid glycoside that primarily targets NF-κB and Nrf2/Keap1 signaling pathways. This compound exhibits significant cardioprotective and hypoglycemic properties, regulating glucose metabolism and modulating lipid profiles. Research applications include the study of diabetic cardiomyopathy, type 2 diabetes, atopic dermatitis, tumors, and atherosclerotic diseases. Additionally, Esculeoside A inhibits dendritic cell maturation and T-cell proliferation, and exhibits anti-tumor activity against breast cancer and melanoma cells. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
NF-κB Inhibitor
Ergolide is a selective NF-κB/p65 and NLRP3 inhibitor that effectively disrupts the NF-κB signaling pathway and inhibits the nuclear translocation of p65. By irreversibly binding to the NACHT domain of NLRP3, Ergolie suppresses inflammasome assembly, significantly reducing the production of inflammatory mediators such as NO and PGE2. This compound promotes apoptosis in cancer cells, induces autophagy, and generates reactive oxygen species (ROS). Ergolide also enhances the therapeutic efficacy of vincristine and has been shown to alleviate acute lung injury in models of sepsis and inflammation, contributing to research in metastatic uveal melanoma, neurodegenerative diseases, and acute lymphoblastic leukemia. -
Apoptosis Inducer
Andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent. -
HDAC inhibitor
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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HDAC Inhibitor
Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent. -
HDAC inhibitor
Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. - Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
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IKK2/IKK complex/IKK1 inhibitor
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. -
HDAC inhibitor
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM. -
HDAC inhibitor
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts. -
mitochondria-targeted antioxidant
Demethyleneberberine is a natural mitochondria-targeted antioxidant. -
Autophagy inducer
Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans. -
NF-κB inhibitor
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass. -
traditional Chinese medicines
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca2+-influx blocker. -
antithyroid agent
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2. -
antiinflammation agent
Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. -
HDAC6 inhibitor
Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. -
pan-HDAC inhibitor
Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity. -
anticancer agent
Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways. -
NF-κB inhibitor
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. -
NF-κB inhibitor
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. -
PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ. -
NF-κB inhibitor
Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor. -
NF-κB inhibitor
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect. -
HDAC inhibitor
CG-200745 is a potent HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket.
