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  • Inhibitors & Agonists
    1693
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Eupalinolide A
T5826877822-40-7
Eupalinolide B is a natural product ,and demonstrates potent cytotoxicity against A-549, BGC-823, SMMC-7721, and HL-60 tumour cell lines.
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Ponasterone A
AI3-44686
T2120513408-56-5
Ponasterone A is an ecdysteroid with high affinity for the ecdysteroid receptor. It enables rapid switching on and off of reporter genes and is a potent regulator of gene expression in cells and transgenic animals.
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6-8 weeks
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Polyphyllin I
T389550773-41-6
Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.
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TargetMol | Inhibitor Hot
TargetMol | Citations Cited
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2',3'-cGAMP sodium
2'-3'-cyclic GMP-AMP sodium
T10065L2734858-36-5In house
2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.
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S-Allylmercaptocysteine
T744142281-22-3In house
S-Allylmercaptocysteine (SAMC) is an organic sulfur compound extracted from garlic, with anti-cancer, anti-inflammatory, and antioxidant properties. It protects against hepatocellular damage, improves alcoholic liver disease by modulating insulin receptor signaling, and enhances anti-tumor immunity by inhibiting PD-L1 expression.
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Praeruptorin B
Praeruptorin D
T4S142173069-28-0In house
Praeruptorin B (Praeruptorin D), a compound found in the roots of Peuced, is an inhibitor of sterol regulatory element-binding proteins (SREBPs) that attenuates the metastatic ability of human renal cancer cells by targeting CTSC and CTSV expression, and can be used in the study of osteoporosis.
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7-10 days
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Nothofagin
TN199611023-94-2In house
Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases.
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8-10 weeks
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Phanginin A
T730741011528-58-7In house
Phanginin A, a potent and orally active activator of salt-induced kinase 1 (SIK1), effectively inhibits gluconeogenesis, increases the expression of p-SIK1, and decreases the expression of p-CREB. By reducing blood glucose levels and enhancing glucose tolerance and dyslipidemia, Phanginin A holds potential for type 2 diabetes research.
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(S)-Coriolic acid
13(S)-HODE
T3797429623-28-7In house
(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.
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6-8 weeks
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Hydrangenol
TN4234480-47-7In house
Hydrangenol is a natural product and can be isolated from Hydrangea serrata leaves. Hydrangenol is an antiphotoaging compound with oral activity. Hydrangenol can reduce MMP and inflammatory cytokine expression and increase moisturizing factors and antioxidant genes level, result in preventing wrinkle formation.
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Imperatorin
Ammidin, 8-Isoamylenoxypsoralen, 8-Isopentenyloxypsoralene, Marmelosin, Pentosalen
T2845482-44-0
Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.
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Bisdemethoxycurcumin
Curcumin III, Didemethoxycurcumin
TL000724939-16-0
Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt β-catenin pathway, and inhibits LPS induction of iNOS expression [3].
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Tetrahydroxystilbene-2-O-β-D-glucoside
tetrahydroxyl diphenylethylene-2-o-gluco, EH-201
T495655327-45-2
Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.
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TargetMol | Citations Cited
Catalase
T192299001-05-2
Catalase is an essential enzyme in the metabolism of H2O2 and reactive oxygen species (ROS). The expression and localization of Catalase are markedly altered in tumors.
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4-6 weeks
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Estradiol
β-Estradiol, E2, 17β-Oestradiol, 17β-Estradiol
T104850-28-2
Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).
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TargetMol | Citations Cited
α-Terpineol
Terpineol
Fr1411598-55-5
Terpineol possesses antifungal activity against Trichophyton mentagrophytes, it also exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria. α-Terpineol (Terpineol) shows anticonvulsant, and anti-inflammatory activities, it inhibits the gene expression of the IL-6 receptor.
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5,6-Benzoflavone
β-Naphthoflavone, beta-NF
TN66946051-87-2
5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT Nrf-2 HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.
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(-)-(S)-Equol
4',7-Isoflavandiol, (−)-Equol, Equol, 4',7-Dihydroxyisoflavan
T6491531-95-3
(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.
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β-Glycerophosphate disodium salt hydrate
T4915154804-51-0
β-Glycerophosphate is a classical serine-threonine phosphatase inhibitor used in kinase reaction buffers. BGP is often used in combination with other phosphatase protease inhibitors for broad spectrum inhibition. It functions as an organic phosphate donor
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Hederagenin
Hederagenol, Hederagenic acid, Caulosapogenin, Astrantiagenin E
T3039465-99-6
Hederagenin (Hederagenol) is a triterpenoid saponin inhibiting LPS-stimulated expression of iNOS, COX-2, and NF-κB.
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3-Carene
Delta-3-Carene
T1010913466-78-9
3-Carene(Delta-3-Carene) is a bicyclic monoterpene extracted from western larch and Douglas-fir that acts as a phytofungicide.3-Carene inhibits inflammatory infiltrates and COX-2 overexpression induced by nociceptive stimuli.3-Carene has anti-injury properties and promotes the activity and expression of alkaline phosphatase, an early marker of osteoblast differentiation.
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7-10 days
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Methyl eugenol
4-allylveratrole, eugenyl methyl ether, O-methyleugenol, Eugenol Methyl ether
T3S225993-15-2
1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.
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L-Ascorbic acid 2-phosphate
2-Phospho-L-ascorbic acid
T1939023313-12-4
L-ascorbic acid 2-phosphate (Vitamin C phosphate) is a stable and long-lasting vitamin C derivative that stimulates collagen formation and has potential antioxidant capacity. L-ascorbic acid 2-phosphate is commonly used to promote osteogenic differentiation of human adipose stem cells (hASCs) in cell culture by increasing alkaline phosphatase (ALP) activity and runt-related transcription factor-2-DNA(runx2A) expression.
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1-2 weeks
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Sodium taurocholate
Taurocholate Sodium
TWA2417145-42-6
Sodium taurocholate (Taurocholate Sodium) hydrate is the main end product of cholesterol catabolism. During enterohepatic circulation, bile taurocholic acid is converted by the microorganisms to taurodeoxycholic acid and deoxycholic acid.[3] These are reabsorbed by the liver via a carrier-mediated process and converted by liver enzymes to taurocholic acid.
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