Biologically Active Small Molecules
-
Docosahexaenoyl Ethanolamide
Cayman ChemicalThe ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…
-
8-iso Prostaglandin F1ß
Cayman Chemical8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.
-
Benzydamine Hydrochloride
LKT LabsBenzydamine is a non-steroidal anti-inflammatory drug (NSAID) that also exhibits analgesic, anesthetic, and antibacterial activities. Benzydamine is clinically used to treat mucositis and sore throat. Unlike most NSAIDs, benzydamine inhibits prostaglandin synthetase, not cyclooxygenase (COX).
-
Vitexin
Cayman ChemicalAn apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.
-
NF449 (sodium salt)
Cayman ChemicalAn analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to…
-
EA4
Cayman ChemicalA quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.
-
Methsuximide
Cayman ChemicalA succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.
-
GDC-0152
Cayman ChemicalA potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.
-
2,3-bis (4-Hydroxyphenyl) Propionitrile
Cayman ChemicalAn ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.
-
DBIBB
Cayman ChemicalA non-lipid agonist of LPA2 (EC50 = 0.10 µM) that is without effect at other LPA receptor subtypes; protects IEC-6 cells against caspase activation and apoptosis following irradiation; increases the survival of mice suffering from hematopoietic acute radiation syndrome after…
-
EGFR Inhibitor
Cayman ChemicalA cell permeable, selective inhibitor of the EGFR kinase (IC50s = 21, 63, and 4 nM for EGFR and the L858R and L861Q EGFR mutants, respectively).
-
INT-777
Cayman ChemicalAn agonist of TGR5 (EC50 = 0.82 µM); stimulates the secretion of GLP-1 in mice when given orally (30 mg/kg) after a glucose challenge, particularly when given with a DPP4 inhibitor; increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to…
-
Antimycin A
LKT LabsAntimycin A was initially produced by Streptomyces. Antimycin A binds cytochrome c reductase, inhibiting electron transport chain activity, oxidative phosphorylation, and ATP synthesis. Antimycin A is used in research models to study mitochondrial respiration and superoxide production. Grade: ≥98%
-
Fialuridine
Cayman ChemicalA nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).
-
n-Triacontanol
Cayman Chemicaln-Triacontanol is a plant growth regulator found in the plant cuticle waxes and in beeswax as the palmitate ester. n-Triacontanol has been reported to have growth enhancing properties when applied to the leaves of growing plants.
-
Oxymatrine
Cayman ChemicalA natural alkaloid with antiviral properties, inhibiting the replication of hepatitis B alone and in combination with lamivudine; prevents fibrosis in a number of organs including liver, at least in part by interfering with TGF-β signaling.
-
ML-228
Cayman ChemicalAn activator of the HIF signaling pathway, as demonstrated by HRE reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM); activity is blocked by excess iron,…
-
BCATc Inhibitor 2
Cayman ChemicalA sulfonyl hydrazide that inhibits BCATc (IC50s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC50 = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…
-
CAY10566
Cayman ChemicalA potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.
-
(±)11-HETE
Cayman ChemicalOne of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid.
-
(±)12-HpETE
Cayman Chemical(±)12-HpETE is one of the six monohydroperoxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid (Item No. 90010) and consists of an equal mixture of the R and S isomers. Reduction of the hydroperoxide yields the more stable hydroxyl fatty acid (±)12-HETE (Item…
-
DPTA NONOate
Cayman ChemicalA NO donor with a half-life of three hours at 37°C, pH 7.4; liberates two moles of NO per mole of parent compound.
-
Estrone
Cayman ChemicalEstrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum…
-
Stearic Acid
Cayman ChemicalA long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.
-
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.
-
D-myo-Inositol-3,4,5,6-tetraphosphate (sodium salt)
Cayman ChemicalD-myo-Inositol-3,4,5,6-tetraphosphate (sodium salt) (Ins(3,4,5,6)-P4) is one of several different inositol oligophosphate isomers implicated in signal transduction. It almost completely inhibits calcium-activated chloride channels at a concentration of 8-10 µM. Related inositol…
-
(±)18-HETE
Cayman ChemicalThe racemic version of a CYP450 metabolite of arachidonic acid that dose-dependently stimulates vasodilation of the rabbit kidney.
-
Minocycline (hydrochloride)
Cayman ChemicalA broad-spectrum tetracycline antibiotic which has a particularly long half-life in serum; commonly used in the treatment of acne in older patients; also has both anti-inflammatory and neuroprotective actions.
-
PAF C-16 Carboxylic Acid
Cayman ChemicalModified with a carboxylic acid group terminating the C-16 alkyl chain, providing a convenient site for chemical crosslinking.
-
Jacaric Acid
Cayman ChemicalA conjugated PUFA that induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM); increases the production of ROS, leading to oxidative stress that contributes to cytotoxicity.
-
HA-155
Cayman ChemicalA selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.
-
18ß-Glycyrrhetinic Acid
Cayman ChemicalA major metabolite of glycyrrhizin, a constituent of licorice that exhibits anti-ulcerative, anti-inflammatory, and immunomodulatory properties; at 100 mg/kg/day, reduces lipid peroxidation and increases antioxidant activity in diabetic rats; suppresses LPS-induced TNF-α production and…