Biologically Active Small Molecules
-
Gallic Acid
Cayman ChemicalA trihydroxybenzoic acid that demonstrates antioxidant activity by scavenging DPPH• and HO• (IC50s = 9.4 and 191 μM, respectively) and inhibiting microsomal lipid peroxidation (IC50 = 1.51 μM).
-
Cinaciguat (hydrochloride)
Cayman ChemicalAn activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.
-
Aminoguanidine (hydrochloride)
Cayman ChemicalAminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS. The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively. Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.
-
11ß-Prostaglandin E2
Cayman Chemical11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…
-
-
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…
-
Baricitinib
Cayman ChemicalAn orally bioavailable, reversible inhibitor of JAK1 and JAK2 (IC50s = 5.9 and 5.7 nM, respectively) that has been shown to inhibit cytokine-induced phosphorylation of STAT3 in healthy human volunteers.
-
Oleoyl Ethanolamide-d4
Cayman ChemicalAn internal standard for the quantification of OEA by GC- or LC-MS.
-
Garcinol
Cayman ChemicalAn inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.
-
AM404
Cayman ChemicalAn analog of AEA that potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons; selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis; inhibits the transport of AEA with an IC50 value of 1 µM in rat…
-
AZD 1080
Cayman ChemicalA potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist MK-801.
-
Bongkrekic Acid
LKT LabsBongkrekic acid is an antioxidative compound that inhibits mitochondrial respiration by preventing the mitochondrial permeability transition (MPT); it suppresses transport of ADP/ATP across the mitochondrial inner membrane, decreasing oxidative stress. Grade: ≥98%
-
Spermine NONOate
Cayman ChemicalSpermine NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 39 minutes and 230 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.
-
Bulleyaconitine A
LKT LabsBulleyaconitine A (BLA) is found in Aconitum bulleyanum and exhibits analgesic and anesthetic activity. BLA has been used as a treatment for a variety of pain-related and inflammatory disorders. BLA inhibits voltage-gated Na+ channels in a use-dependent manner, reducing peak Na+ currents during…
-
(±)8(9)-EET methyl ester
Cayman ChemicalA derivative of (±)8(9)-EET which is stable enough to ship and handle routinely.
-
CAY10499
Cayman ChemicalCAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.
-
LY223982
Cayman ChemicalA potent LTB4 receptor antagonist that inhibits the specific binding of [3H]-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM; inhibits the LTB4-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.
-
Bromocriptine (mesylate)
Cayman ChemicalA potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.
-
Thiomuscimol
Cayman ChemicalA GABAA receptor agonist (IC50 = 19 nM) that has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
-
N-nonanoyl-L-Homoserine lactone
Cayman ChemicalA small diffusible signaling molecule produced by wild-type E. carotovora strain SCC 3193 involved in quorum sensing, controlling gene expression, and affecting cellular metabolism.
-
XE 991 (hydrochloride)
Cayman ChemicalA blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC50 = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC50 = 0.6 µM); shows good in vivo potency and duration of action.
-
(R)-Equol
Cayman ChemicalAn ER agonist that binds to ERα and ERβ with Ki values of 27.4 and 15.4 nM, respectively; demonstrates higher ER agonist activity at ERα compared to ERβ (EC50 = 66 and 330 nM, respectively).
-
N-Acetyl-D-Leucine
LKT LabsN-acetyl-D-leucine is a D-amino acid that is deacylated in bacteria by d-aminoacylase enzymes. D-amino acids inhibit bacterial biofilm formation when they are incorporated into the cell wall. Compounds such as N-acetyl-D-leucine induce release of amyloid fibers that link cells together in the…
-
Cholesterol
MP BiomedicalsCholesterol is the principal sterol of the higher animals, found in all body tissues. It is the main constituent of gallstones and all biological membranes. Approximately 25% of total brain lipid is cholesterol. Cholesterol is suitable for use in liposome preparations.
-
3'-Sialyllactose (sodium salt)
Cayman ChemicalAn abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.
-
Monobromobimane
Cayman ChemicalA thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.
-
Cinnabarinic Acid
Cayman ChemicalA partial receptor agonist of mGlu4, effective at 100 µM, with no activity at other mGlu receptor subtypes; induces apoptosis of T cells at 300-500 µM.
-
(±)-Jasmonic Acid
Cayman ChemicalA plant growth regulator involved in the signaling mechanisms for a variety of conditions including plant defense, wound healing, tuberization, fruit ripening, and senescence.
-
(±)18-HETE
Cayman ChemicalThe racemic version of a CYP450 metabolite of arachidonic acid that dose-dependently stimulates vasodilation of the rabbit kidney.
-
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.
-
Aminoethoxyvinyl Glycine (hydrochloride)
Cayman ChemicalAn inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs; reduces ethylene-mediated plant changes in growth and development; inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.
-
n-Dodecyl-ß-D-maltoside
Cayman ChemicalA non-ionic detergent commonly used to solubilize membrane-associated proteins; helps retain the native conformation and activity of membrane-associated proteins, and facilitates the reforming of these proteins after denaturation.