NF-κB Modulator

Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.

Cibinetide (ARA290) is a non-hematopoietic Erythropoietin analog. Cibinetide selectively activates the EPOR/CD131 heteromer IRR without activating EPOR homodimers, and exerts neuroprotective effects through β-common receptor signaling. Cibinetide inhibits Cathepsin K/OSCAR/OC-STAMP/DC-STAMP/NFATC1, increases OPG and Alkaline phosphatase, and decreases CD115. Cibinetide modulates SIRT1/NF-κB/IL-1β signaling, reduces inflammatory infiltration and periapical bone loss, protects pancreatic islets, reduces IBMIR-related platelet consumption, and prolongs graft function. Cibinetide extends healthspan and attenuates age-related cardiac and body weight decline. Cibinetide can be used in research on cerebral ischemic stroke, sarcoidosis-associated small fiber neuropathy, and type 1 diabetes.

TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.

Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin.

α-MSH (11-13) (ACTH-(11-13)) acetate is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) acetate exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) acetate also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) acetate can be used in research related to traumatic brain injury, fever, and bacterial infections.

Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis.

DpC is an orally active iron chelator and anticancer agent. DpC induces lysosomal membrane permeabilization, redox-active iron/copper complex formation, oxidative stress, and Apoptosis through carrier/receptor-mediated uptake and Pgp-mediated lysosomal transport, while upregulating NDRG1 to inhibit oncogenic signaling and tumor progression, and modulates pathways such as JNK, IκBα/NF-κB, c-Src, and EGFR/HER2/HER3. DpC selectively inhibits tumor cell proliferation and can be used in research on neuroblastoma, kidney disease, prostate cancer, and pancreatic cancer.

RSM3 is a METTL3-METTL14 complex inhibitor with a K_d of 3.10 μM for the METTL3-METTL14 complex. RSM3 reduces the m⁶A modification level of SLC31A1 and the global RNA methylation level. RSM3 upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 is applicable to the research of preeclampsia and cancer.

Lariciresinol is an orally active ingredient. Lariciresinol can be isolated from Arabidopsis thaliana. Lariciresinol inhibits α-glucosidase activity (IC₅₀ of 6.97 μM; K_i of 0.046 μM). Lariciresinol dereases Bcl-2, upregulates Bax and induces Apoptosis. Lariciresinol regulates TGF-β and NF-κB pathways. Lariciresinol has antitumor activity against liver cancer, gastric cancer, and breast cancer. Lariciresinol shows antifungal activity and anti-diabetic activity.

Betulinic acid (Standard) is the analytical standard of Betulinic acid. This product is intended for research and analytical applications. Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.

AEOL-10150 pentachloride is a metalloporphyrin-catalyzed antioxidant and a superoxide dismutase mimetic. AEOL-10150 pentachloride scavenges ROS and RNS, and modulates the NF-κB signaling pathway. AEOL-10150 pentachloride has potent antioxidant and anti-inflammatory activities. AEOL-10150 pentachloride effectively mitigates tissue damage caused by radiation and chemical agents such as CEES (HY-W199190). AEOL-10150 pentachloride synergizes with radiotherapy to exert anticancer effects on prostate tumors.

GQ-16 is an orally active PPARγ partial agonist with an IC₅₀ of 1.84 μM and a K_i of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer.

Beloranib (ZGN-440; ZGN-433 free base; CKD-732 free base) is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib can be used in research on obesity and hypothalamic obesity.

Girolline (RP 49532) is a protein synthesis inhibitor and a functional modulator of eIF5A. Girolline induces ribosome stalling by interfering with the binding of eIF5A to ribosomes. Girolline also inhibits the production of IL-6 and IL-8, and induces cell cycle arrest in tumor cells. Girolline is applicable to research related to inflammatory diseases, solid tumors, leukemia and malaria.

Bacoside A is an orally active, blood-brain barrier-permeable triterpenoid saponin that modulates the activities of ATPases, AChE, CaMK2A and iNOS. Derived from Bacopa monniera. Bacoside A exerts significant antioxidant, anti-inflammatory and anti-apoptotic effects by maintaining ion balance, scavenging reactive oxygen species, stabilizing cell membranes, and regulating the expression of NF-κB and apoptosis-related proteins. Bacoside A counteracts morphine-induced reductions in Na⁺/K⁺-ATPase, Ca²⁺-ATPase and Mg²⁺-ATPase activities, increases mitochondrial membrane potential, and decreases intracellular reactive oxygen species levels. Bacoside A specifically binds to calcium/calmodulin-dependent protein kinase IIA to trigger endoplasmic reticulum calcium release. Bacoside A exhibits non-apoptotic cytotoxicity against glioblastoma cells while protecting normal nerve cells from stress-induced damage. Bacoside A is applicable to the research of Parkinson's disease and glioblastoma multiforme.

Benzylurea is an anti-inflammatory agent. Benzylurea inhibits LPS (HY-D1056)-induced upregulation of MTCH2 expression and regulates pathways associated with mitochondrial function, inflammation and cell survival. Benzylurea alleviates LPS-induced proliferation inhibition and apoptosis of periodontal ligament fibroblasts, as well as the release of proinflammatory cytokines. Benzylurea can be used in studies related to periodontitis.

4-PSQ is an orally active neuroprotective agent. 4-PSQ possesses both antioxidant and anti-inflammatory activities. 4-PSQ improves cognitive impairment and depressive- and anxiety-like emotional abnormalities in mice by regulating the activity of Na⁺, K⁺-ATPase, the NFκB signaling pathway, and the expression of p21. 4-PSQ can be used for the research of neurological diseases.

DpC hydrochloride is an orally active iron chelator and anticancer agent. DpC hydrochloride induces lysosomal membrane permeabilization, redox-active iron/copper complex formation, oxidative stress, and Apoptosis through carrier/receptor-mediated uptake and Pgp-mediated lysosomal transport, while upregulating NDRG1 to inhibit oncogenic signaling and tumor progression, and modulates pathways such as JNK, IκBα/NF-κB, c-Src, and EGFR/HER2/HER3. DpC hydrochloride selectively inhibits tumor cell proliferation and can be used in research on neuroblastoma, kidney disease, prostate cancer, and pancreatic cancer.

S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC₅₀ value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.

Swertiamarin (Standard) is the analytical standard of Swertiamarin. This product is intended for research and analytical applications. Swertiamarin is an orally active iridoid compound with hypoglycemic, hypolipidemic, anti rheumatic and antioxidant activities, which can be used in the research of diabetes and arthritis.