nf-κb p65

1-(b-D-Xylofuranosyl)-N6-(p-methoxybenzyl) adenine is a Nucleoside Derivative - Xylo-nucleoside, 6-Modified purine nucleoside.

Nucleoside Derivatives - Fluoro-modified nucleoside; Halo-nucleoside

6-O-p-Coumaroyl-1,2-di-O-galloyl-b-D-glucopyranose is a useful organic compound for research related to life sciences and the catalog number is T130064.

4-Amino-6-bromo-5-cyano-1-(3-deoxy-3-fluoro-2-O-acetyl-5-(O-p-toluoyl)-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine is a useful organic compound for research related to life sciences and the catalog number is TNU1038.

4-Chloro-5-iodo-7-(2-deoxy-3,5-bis-O-(p-toluoyl)-b-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine is a useful organic compound for research related to life sciences and the catalog number is TNU1024.

1-O-Cinnamoyl-6-O-p-coumaroyl-b-D-glucopyranose is a useful organic compound for research related to life sciences and the catalog number is T130425.

4-Chloro-7-(2-deoxy-3,5-bis-O-(p-toluoyl)-b-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine is a useful organic compound for research related to life sciences and the catalog number is TNU1021.

Nucleoside Derivatives - 7-Deaza-8-aza-purine nucleosides; 6-Modified purine nucleosides

Nucleosides and Reagents - Fluoro-modified nucleoside; pyridine nucleoside

1-(β-D-Xylofuranosyl)-N6-(p-methoxybenzyl) adenine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms include the inhibition of DNA synthesis and the induction of apoptosis, among others [1].

1-(a,b)-O-methyl-3,5-di-(O-p-toluoyl)-2-deoxy-D-ribose is a Carbohydrate derivative.

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Schisantherin A (Wuweizi ester-A) is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera, has been used as an antitussive, tonic, and sedative agent.

Sinapinic Acid (Synapoic acid) protects the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid with antioxidant role protects cardiac cells and its functions from I/R induced oxidative stress. Sinapic acid is a potentially useful agent for the protection against liver fibrosis and cirrhosis. Sinapic acid prevents the alterations in the levels of lipids and lipoproteins by virtue of its anti-lipidaemic effect in isoproterenol induced myocardial infarcted rats. Sinapic acid ameliorates hyperglycemia through PLC-PKC signals to enhance the glucose utilization in diabetic rats.

CORM-3 is a carbon monoxide-releasing molecule with anti-inflammatory and cardioprotective activity.

Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotective potential against myocardial is

JSH-23, an NF-κB inhibitor（IC50= 7.1 μM）, suppresses the transcriptional activity.

SC75741 is a potent P65 inhibitor with IC50 of 200 nM

Mangiferin (Hedysarid) is used for antidiabetes. Extracted from Mangifera indica L.

Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) is an antioxidant compound used in the treatment of oxidative stress and related afflictions.

Maslinic acid (Crategolic acid) is a DNA polymerase B inhibitor.

Anti-inflammatory agent 65 (compound 29), a Hederagonic acid derivative, exhibits potent activity by inhibiting nitric oxide (NO) release, nuclear translocation of IRF3 and p65, and disrupting the STING/IRF3/NF-κB signaling pathway, thus attenuating the inflammatory response [1].

Isomerazin (Isomeranzin) has anti-inflammatory activity, it suppresses inflammation by inhibiting M1 macrophage polarization through the p65, NF-κB and ERK pathway.

Grasshopper ketone, isolated from the brown alga Sargassum, is a potent inhibitor of LPS-induced NO production in RAW 264.7 cells and induces anti-inflammatory effects by inhibiting MAPK (ERK, JNK and p38) and NF-κB p65 phosphorylation.

Helenalin is a selective inhibitor of transcription factor NF-κB by direct targeting of p65. It is an anti-inflammatory sesquiterpene lactone compound with alkylating activity. Through its ability to target the cysteine sulfhydryl groups in the p65 subunit of NF-κB, helenalin effectively inhibits its DNA binding.

EP12, a c-Myc inhibitor and G4 stabilizer, induces apoptosis and DNA damage in multiple myeloma cells while obstructing P65/P50 nuclear translocation by disrupting the NF-κB signaling pathway, effectively inhibiting multiple myeloma growth [1].

SRTCX1002 is a SIRT1 Activator Suppressing Inflammatory Responses through Promotion of p65 Deacetylation and NF-κB Activity inhibitor.

HD-TAC7, a potent PROTAC HDAC degrader, exhibits IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM for HDAC1, HDAC2, and HDAC3, respectively. It effectively decreases NF-κB p65 in RAW 264.7 macrophages and is utilized in research targeting inflammatory diseases such as asthma and chronic obstructive pulmonary disease (COPD) [1].

ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression through inhibition of NF-κB activation, inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR, and inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR. ACHKP has anti-HIV-1 activity and inhibits TNF-α-induced recruitment of NF-κB (p65) to the HIV-1 LTR.

Rubiadin-1-methyl ether (Rubiadin 1-methyl ether) is a natural product.It inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.

IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.

TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor exhibiting a dissociation constant (K D) of 12.06 μM. By binding to TNF-α, it impedes TNF-α-induced caspase activation and the NF-κB signaling pathway. Additionally, it suppresses the phosphorylation of IκBα and the nuclear migration of NF-κB p65. This compound is utilized in the study of TNF-α-mediated autoimmune diseases [1].

1. Cucurbitacin IIb is one of the major active compounds in Hemsleyadine tablets which have been used for clinical treatment of bacillary dysentery, enteritis and acute tonsilitis. 2. Cucurbitacin IIb exhibits its anti-inflammatory activity through modula

SB26019 is a potent anti-neuroinflammatory compound that modulates the activation of NF-κB by promoting the formation of monomeric α-tubulin. This action of SB26019, in turn, hinders the translocation of p65, signifying its regulatory effect on neuroinflammatory processes [1].

TD1092, a pan-IAP degrader, effectively degrades cIAP1, cIAP2, and XIAP, catalyzing the activation of Caspase 3/7 and fostering apoptosis in cancer cells through IAP degradation. It also obstructs the TNFα-mediated NF-κB pathway, diminishing the phosphorylation of IKK, IkBα, p65, and p38, and operates as a PROTAC. This compound is utilized in cancer research [1].

Anti-inflammatory agent 6 exhibits anti-inflammatory potential by blocking the phosphorylation of Iκb kinase α/β (IKKα/β), IκBα and nuclear factor kB p65 (NF-κb p65), which are key controllers of inflammation.

Anemarsaponin B has anti-inflammatory effect in LPS-treated RAW 264.7macrophages, the effect is associated with the inhibition of NF-κB transcriptional activity, possibly via the p38 MAP kinase pathway. Anemarsaponin B can inhibit PAF-induced rabbit platelet aggregation in vitro.

F1, an anti-inflammatory peptide, incorporates the HIV-1 Tat protein transduction domain linked with a 15-amino acid sequence from residues 46-60 of the inhibitor of NF-κB kinase-interacting peptide (IKIP). It effectively blocks LPS-induced phosphorylation of IκB kinase α (IKKα) and IKKβ, along with the nuclear translocation of NF-κB (p65) in mouse peritoneal macrophages at 5 µM concentration. F1, administered at 5 mg/kg in vivo, significantly reduces IL-6, TNF-α, and IL-1β serum levels and enhances survival in a mouse sepsis model induced by LPS.

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

Avicularin (Fenicularin) has anti-allergic, anti-inflammatory, hepatoprotective, antioxidant, anti-tumor and other activities. It ameliorates human hepatocellular carcinoma by modulating the activities of NF-κB(p65), COX-2, and PPAR-γ. In LPS-stimulated RAW 264.7 macrophages, it exerts anti-inflammatory activity by inhibiting the ERK signaling pathway.

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 μM). CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1/2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abolishes the TNF-α-induced nuclear translocation of NF-κB/p65 in RAW264.7 cells[1].Benpyrine only blocks cell death induced by TNF-αWT and Y119A, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect L57A- and Y59L-induced cytotoxicity in L929 cells[1]. Benpyrine (25-50 mg/kg; oral gavage; daily; for 2 weeks; Balb/c mice) treatment significantly relieves the symptoms of collagen-induced arthritis. Benpyrine dose-dependently decreases the levels of proinflammatory cytokines, such as IFN-γ, IL-1β and IL-6, and increases the concentration of the anti-inflammatory cytokine IL-10[1].Endotoxemia murine model shows that Benpyrine (25 mg/kg) could attenuate TNF-α-induced inflammation, thereby reducing liver and lung injury[1]. [1]. Weiguang Sun, et al. Discovery of an Orally Active Small Molecule TNF-α Inhibitor. J Med Chem. 2020 Jul 15.

HMGB1-IN-2 (compound 15) is a selective inhibitor of the highly conserved nuclear protein HMGB1, demonstrating no inhibitory effect at an IC50 of 20.2 μM in RAW264.7 cells. At a concentration of 30 μM, HMGB1-IN-2 reduces IL-1β, TNF-α, and caspase-1 p20 levels, and inhibits NF-κB p65 phosphorylation, providing anti-apoptotic effects. In vivo, HMGB1-IN-2 at a dose of 15 mg/kg administered intraperitoneally alleviates kidney injury in a mouse model of septic acute kidney injury. Furthermore, it inhibits Huh7 and A549 cells with IC50 values of 77.0 μM and 82.0 μM, respectively [1].

NF-κB-IN-11 (Compound 3i) is an inhibitor of NF-κB, effectively blocking TNF-α-induced NF-κB pathway activation and the nuclear translocation of NF-κB. It also reduces the expression levels of phospho-IKK, IκBα, and NF-κB p65. Demonstrating anti-inflammatory properties, NF-κB-IN-11 mitigates dextran sulfate sodium-induced colitis in mice and exhibits a maximum tolerated dose (MTD) exceeding 1852 mg/kg in acute toxicity assays when administered orally (p.o.) [1].

Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α and PPARγ agonist. In vivo, gemfibrozil reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol.

3,3-Dimethyl-1-butanol (DMB) is an orally active compound that inhibits trimethylamine (TMA) and trimethylamine N-oxide (TMAO), along with the signaling pathways of p65 NF-κB and TGF-β1/Smad3. It holds potential for use in preventing or treating cardiovascular disease (CVD).

SRTCX1003, a SIRT1 activator, suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity.

SN50 TFA is a cell-permeable inhibitor of NF-κB and attenuates alveolar hypercoagulation and fibrinolysis inhibition in acute respiratory distress syndrome mice through inhibiting NF-κB p65 translocation. SN50 TFA can be used in studies about ARDS.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways.