Biologically Active Small Molecules
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STK393606
Cayman ChemicalA selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC50 = 26.4 nM; Ki = 5 nM).
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Ro 61-8048
Cayman ChemicalA potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine to 3-hydroxy kynurenine; reduces ischemia-mediated neuronal damage in tissues; can be used in vivo by direct injection.
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8-iso-15-keto Prostaglandin F2ß
Cayman ChemicalA potential metabolite of 8-iso PGF2β via the 15-hydroxy PGDH pathway.
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Bicyclo Prostaglandin E2
Cayman ChemicalBicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…
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Rosiglitazone (potassium salt)
Cayman ChemicalA potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.
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D-AP5
Cayman ChemicalA selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.
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DMABA-d4 NHS ester
Cayman ChemicalDMABA-d4 NHS ester is intended for use in combination with DMABA NHS ester (Item No. 11216) as a derivatizing reagent for PE lipids in order to facilitate MS characterization and to quantify relative changes in their abundance.
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CH5132799
LKT LabsCH5132799 is an inhibitor of PI3K that is somewhat selective for p110a isoforms. This compound exhibits anticancer chemotherapeutic activity, inhibiting cell proliferation and tumor growth in breast cancer, ovarian cancer, prostate cancer, and endometrial cancer models.
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Prostaglandin B2
Cayman ChemicalPGB2 is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 µg/kg).
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Manumycin A
Cayman ChemicalA potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity: inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation; inhibits IKK in an number of cells types.
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CAY10512
Cayman ChemicalCAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.
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Angiotensin Fragment 1-7 (acetate)
Cayman ChemicalAn angiotensin metabolite that functions as a type 1 angiotensin II receptor agonist whereupon it can control hydroelectrolyte balance and demonstrates vasodilatory and anti-inflammatory actions in opposition to various adverse effects of angiotensin II.
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Rosiglitazone
Cayman ChemicalA potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.
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Ampkinone
Cayman ChemicalA small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…
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DAN-1 EE (hydrochloride)
Cayman ChemicalDAN-1 EE is a fluorescent indicator for the bioimaging of NO. DAN-1 EE is a cell permeable derivative of DAN, a molecule which has been used extensively in the quantitation of nitrate and nitrite using fluorescence spectroscopy. Upon entry into the cell, DAN-1 EE is transformed into the less cell…
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PF-670462 (hydrochloride)
Cayman ChemicalA potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively); less effectively inhibits a wide variety of related or common kinases; disrupts circadian rhythms in cells and animals; blocks the locomotor response to amphetamines in mice.
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SMER3
Cayman ChemicalA selective inhibitor of SCFMET30 ubiquitin ligase, an E3 ligase that regulates transcription, cell-cycle control, and immune response; at 5 μM, upregulates a set of methionine biosynthesis genes by altering the SCFMET30 complex, preventing ubiquitination of target proteins, including Met4.
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ß-Carotene
LKT Labsß-Carotene is a red-orange terpene pigment originally found in various plants and fruits; it is a prodrug for vitamin A. ß-Carotene exhibits antioxidative, cytoprotective, anticancer, anti-inflammatory, anti-hyperlipidemic, and anti-obesity activities. ß-Carotene is used in research models to…
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Resolvin D3
Cayman ChemicalA DHA-derived product first identified in mouse inflammatory exudates; reduces neutrophil infiltration in vivo in both mouse peritonitis and dermal inflammation; enhances macrophage phagocytosis and efferocytosis.
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Methotrexate
Cayman ChemicalAn analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…
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BzATP (ammonium salt)
Cayman ChemicalAn activator of the P2X receptors that exhibits 5-30-fold greater potency at the P2X7 receptor than ATP; activates the human, rat, and mouse receptors with EC50 values of 0.7, 3.6, and 285 μM, respectively.
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Celecoxib
Cayman ChemicalAn anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.
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WSP-5
Cayman ChemicalA reactive disulfide-containing, fluorescent probe (ex. max 502 nm; em. max 525 nm) designed for fast detection of H2S in biological samples and cells.
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(±)11-HETE
Cayman ChemicalOne of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid.
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Serotonin (hydrochloride)
Cayman ChemicalA monoamine neurotransmitter produced in serotonergic neurons in the CNS and in enterochromaffin cells in the gastrointestinal tract that is important in the regulation of mood, sleep, vomiting, sexuality, and appetite.
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11ß-Prostaglandin F1ß
Cayman ChemicalSteroisomer of PGF1α with both C-9 and C-11 hydroxyls inverted.
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Chrysin
LKT LabsChrysin is a flavone/flavonoid initially found in Passiflora, Oroxylum, and Pleurotis; it is also a byproduct found in propolis. Chrysin exhibits anti-estrogenic, anti-inflammatory, anxiolytic, neuroprotective, cognition enhancing, antioxidative, anti-metastatic, anticancer chemotherapeutic, and…
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ZLN005
Cayman ChemicalA small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…
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Clasto-Lactacystin ß-lactone
Cayman ChemicalActive metabolite of lactacystin, a widely used selective inhibitor of the 20S proteasome, with at least 10 times better activity; irreversibly alkylates subunit X of the 20S proteasome.
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ß-Tocotrienol
Cayman ChemicalAn isomer of Vitamin E that has less potent antioxidant properties than α-tocotrienol.
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ß-Elemene
Cayman ChemicalA natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.