Biologically Active Small Molecules
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[Des-Asp1]-Angiotensin I, Human
LKT LabsAngiotensin I (AT I) is a peptide cleavage product of angiotensin and serves no primary biological purpose other than to function as a precursor to angiotensin II.
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Caffeic Acid
Cayman ChemicalCaffeic acid is an inhibitor of 5-LO with an IC50 value of 3.7-72 µM and 12-LO with an IC50 value of 5.1-30 µM.
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Docosanoyl Ethanolamide
Cayman ChemicalA saturated N-acylethanolamide whose non-CB receptor-mediated pharmacology is still being elucidated; may have a role in the functioning of ion channels.
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ZLN005 (hydrochloride)
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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Butyric Acid Sodium
LKT LabsSodium butyrate is an inhibitor of histone deacetylases (HDACs) that exhibits antidepressant, immunomodulatory, and anticancer activities. In animals undergoing the light dark test, tail suspension test, and forced swim test, sodium butyrate decreases restraint stress-induced depression. In…
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AD57 (hydrochloride)
Cayman ChemicalA polypharmacological cancer therapeutic; potently inhibits RET (IC50 = 2 nM) and reduces the activity of numerous other kinases by more than 80% when given at 1 μM in Drosophila; interferes with kinases downstream of RET, including Src, Raf, and S6K.
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Cylindrospermopsin
Cayman ChemicalA cyanobacterial toxin that targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), inhibits uridine monophosphate synthase complex activity (Ki = 10 µM), and induces DNA damage.
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Leptomycin B
Cayman ChemicalA potent anti-fungal antibiotic that can directly block nuclear transport by inhibiting the action of CRM1.
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HT-2 Toxin
Cayman ChemicalAn active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.
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Isradipine
Cayman ChemicalA selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC50 = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC25 = 0.45 nM); attenuates β-amyloid…
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15(S)-Latanoprost
Cayman ChemicalAn analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC50 value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.
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Benzo[a]pyrene
LKT LabsBenzo[a]pyrene is a polycyclic aromatic hydrocarbon (PAH) originally found in coal tar, cigarette smoke, and wood smoke. Metabolites of this compound bind DNA and induce mutations. Benzo[a]pyrene is highly carcinogenic and is used in research models to induce carcinogenesis and tumor formation.…
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BRD73954
Cayman ChemicalA small molecule inhibitor that potently and selectively inhibits both HDAC6 and HDAC8 (IC50s = 36 and 120 nM, respectively).
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Hydroxy Dimetridazole
Cayman ChemicalA metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.
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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…
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Everolimus
Cayman ChemicalA hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM; orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.
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11-deoxy Prostaglandin E2
Cayman Chemical11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.
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Creatinine-d3
Cayman ChemicalAn internal standard for the quantification of creatinine by GC- or LC-MS.
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Calcein AM
Cayman ChemicalA cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.
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HE-3235
Cayman ChemicalA synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC50 = 6 nM) and in vivo.
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Sodium Valproate
MP BiomedicalsValproic Acid, Sodium Salt is a branched chain fatty acid which is reported to enhance central GABAergic neurotransmission and inhibit Na+ channels. Sodium Valproate is reported to cause inositol depletion, activate the ERK pathway, inhibit GSK-3α and GSK-3β. Valproic Acid has been…
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Azaperone
LKT LabsAzaperone is a butyrophenone tranquilizer that exhibits sedative activity through the inhibition of a-adrenergic receptors. Azaperone also inhibits dopamine receptors and histamine receptors; it also may display antiemetic, antipsychotic, antihistaminergic, and anticholinergic activities.
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(S)-MG132
Cayman ChemicalA potent, reversible, and cell permeable proteasome inhibitor; inhibits cell growth in B16 and IPC227F cells with IC50 values of 42 and 77 nM, respectively; inhibits NF-κB activation, sensitizing a variety of carcinoma cell lines to apoptosis.
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Tafluprost ethyl amide
Cayman ChemicalA more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).
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PtdIns-(1,2-dihexanoyl) (sodium salt)
Cayman ChemicalA synthetic analog of natural PtdIns containing C6:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.
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CAY10678
Cayman ChemicalA benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…
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Griseofulvin
Cayman ChemicalA natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin; alters microtubule dynamics, resulting in metaphase arrest.
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CRT0066101 (hydrochloride)
Cayman ChemicalA pan inhibitor PKD (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively); blocks cell proliferation, induces apoptosis, and reduces the viability of pancreatic cancer cells both in vitro and in vivo.
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Meropenem
Cayman ChemicalAn intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.