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  • Inhibitors & Agonists
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3-Oxo-5β-cholanoic acid
DHLCA, Dehydrolithocholic acid
T135021553-56-6
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.
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6-8 weeks
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Cortisone acetate
Cortisone 21-acetate, NSC 49420
T003450-04-4
Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.
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Tacrolimus monohydrate
FK-506, FR 900506, Prograf, FR900506, Tacrolimus hydrate, LCP-Tacro, FK 506
T20879109581-93-3
Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.
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Vitamin K2
Menatetrenone
T233611032-49-8
Vitamin K2 (Menatetrenone) is a menaquinone compound and form of vitamin K2 with potential antineoplastic activity. Menatetrenone may act by modulating the signaling of certain tyrosine kinases, thereby affecting several transcription factors including c-myc and c-fos. This agent inhibits tumor cell growth by inducing apoptosis and cell cycle arrest.
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Isotretinoin
13-cis-Retinoic acid
T16114759-48-2
Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs), which act as transcription factors that promote cell differentiation and apoptosis. This naturally occurring retinoic acid has potential antineoplastic activity, exhibits immunomodulatory and anti-inflammatory responses, and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.
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TargetMol | Citations Cited
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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Uridine
β-Uridine, Uridin, NSC 20256
T222158-96-8
Uridine (Uridin) is a nucleoside compound, one of the four bases that make up RNA, that replaces thymine in DNA during transcription and pairs with adenine.
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Caffeic Acid Phenethyl Ester
Phenylethyl Caffeate, CAPE
T6429104594-70-9
Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).
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Bufalin
T1719465-21-4
Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic a
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Oroxylin A
6-Methoxybaicalein, Baicalein 6-methyl ether
T6S1315480-11-5
1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.
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Wedelolactone
IKK Inhibitor II
T3384524-12-9
Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.
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Crocin
Gardenia Yellow, Alpha-Crocin
T282342553-65-1
Crocin (Gardenia Yellow) is a water-soluble carotenoid pigment of saffron (Crocus sativus L. ) that has been used as a spice for flavoring and coloring food preparations, and in Chinese traditional medicine as an anodyne or tranquilizer. Crocin suppresses tumor necrosis factor (TNF)alpha-induced apoptosis of pheochromocytoma (PC12) cells by modulating mRNA expressions of Bcl-2 family proteins, which trigger downstream signals culminating in caspase-3 activation followed by cell death. Crocin prevented the activation of nSMase by enhancing the transcription of gamma-glutamylcysteinyl synthase, which contributes to a stable glutathione supply that blocks the activity of nSMase.
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Ouabain octahydrate
G-Strophanthin, Acocantherine
T131811018-89-6
Ouabain octahydrate (Acocantherine) is a cardiac glycoside that inhibits Na(+) K(+) ATPase. Ouabain octahydrate regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.
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Ganoderic acid A
T6S114181907-62-2
1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human
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N4-Acetylcytidine triphosphate
ac4CTP
T194631428903-57-4
N4-Acetylcytidine triphosphate is an efficient substrate for T7 Polymerase-catalyzed in vitro transcription.
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24-Hydroxycholesterol
Cholest-5-ene-3beta,24-diol
T1008630271-38-6
24-Hydroxycholesterol (Cholest-5-ene-3beta,24-diol) is an oxysterol compound that is an activator of the n-methyl-d-aspartate receptor (NMDA) and the transcription factor LXR, which has been used in the study of cardiogenesis and pancreatic cancer.
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Citreorosein
TN1504481-73-2
Citreorosein is a cAMP phosphodiesterase inhibitor, it has anti-inflammatory effect, inhibits proinflammatory cytokines production through the inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation.
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2'-Hydroxychalcone
TN11631214-47-7
2'-Hydroxychalcone is a drug synthesis intermediate for the synthesis of flavonoids. 2'-Hydroxychalcone loaded in nanoemulsion showed fungicidal activity against Coccidioides parapsilosis in Danio rerio model.2'-Hydroxychalcone induced cytotoxicity through oxidative stress in lipid-loaded Hepg2 cells.2'-Hydroxychalcone inhibited the induction of ICAM-1, VCAM-α, tumor necrosis factor-α, and tumor necrosis factor-alpha as determined by reverse transcription-polymerase chain reaction determined by tumor necrosis factor-alpha induces steady-state transcript levels of ICAM-1, VCAM-1, and E-selectin, and therefore may interfere with the transcription of their genes.
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sulforaphane
TQ02074478-93-7
Sulforaphane is a natural isothiocyanate that activates Nrf2 and inhibits AMPK-dependent signaling. Sulforaphane has antitumor and anti-inflammatory activities by increasing the transcription of tumor suppressor proteins and inhibiting histone deacetylase activity.
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fulvotomentoside A
TN6393122739-11-1
Fulvotomentoside A could decrease overexpression of IL-6 and IL-17A, and increase the expression of specific transcription factor Foxp3 of regulatory T cells significantly in intestine. It may be one of the mechanisms that Ful improved intestinal inflamma
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3-O-Methylgallic acid
3,4-Dihydroxy-5-methoxybenzoic acid
TN12373934-84-7
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.
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Calcitroic acid
TN893671204-89-2
Calcitroic acid is a vitamin D receptor (VDR) agonist that activates VDR-mediated transcription. It is the primary metabolite of 1,25-dihydroxyvitamin D3, showing the highest concentrations in the liver and mucosa of mice. The compound exhibits metabolic stability and extremely low toxicity.
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3,5,7,3′,4′-Pentamethoxyflavone
Quercetin 3,5,7,3,4-pentamethyl ether
TN21211247-97-8
3,5,7,3′,4′-Pentamethoxyflavone (Quercetin 3,5,7,3,4-pentamethyl ether) is a natural product that induces adipogenesis in 3T3-L1 preadipocytes by regulating transcription factors during the early stages of differentiation.
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Dehydroleucodine
Dehydroleucodin
TN536936150-07-9
Dehydroleucodine has antidiarrheal, anti-inflammatory, anti-microbial, embryotoxicity, gastric cytoprotective, anti-cancer activities. Dehydroleucodine has an important inhibitory effect in cellular pathways regulating adipocyte differentiation by modulat
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