Biologically Active Small Molecules
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Zidovudine
Cayman ChemicalA nucleoside reverse transcriptase inhibitor that, following triphosphorylation by thymidine kinase, potently blocks replication of HIV (EC50 = 3 nM) with low cytotoxicity (CC50 > 5 μM).
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Mycophenolic Acid ß-D-Glucuronide
Cayman ChemicalThe primary metabolite of mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase that prevents lymphocyte proliferation and activation; typically used as an internal standard for therapeutic drug monitoring analyses of serum or whole blood by HPLC or LC-MS to confirm that patients…
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Genistein
Cayman ChemicalAn isoflavonoid phytoestrogenic compound found in soybeans, pea pods, and other legumes; acts as a tyrosine kinase inhibitor, has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors.
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Chlorzoxazone
Cayman ChemicalA benzoxazolone derivative that causes skeletal muscle relaxation and blocks spasticity in clinical studies; enhances KCa2.2 and KCa3.1 channels (EC50s = 87 and 98 µM, respectively); urinary excretion of its 6-hydroxy metabolite is often used as a probe of CYP2E1 activity in…
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GSK2578215A
Cayman ChemicalGSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…
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4-Methylumbelliferyl 6-thio-Palmitate-ß-D-Glucopyranoside
Cayman ChemicalA fluorogenic substrate of palmitoyl-protein thioesterase.
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Nodularin
Cayman ChemicalA hepatotoxic monocylic pentapeptide that acts as a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively.
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Bromophenol Blue
Cayman ChemicalCommonly used as a pH indicator, a color marker in agarose or polyacrylamide gel electrophoresis, and a dye to detect proteins and nucleic acids (absorbance at 610 nm), particularly when staining living tissues.
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N-(4-Carbethoxyphenyl)retinamide
LKT LabsN-(4-Carbethoxyphenyl)retinamide is a retinoid that exhibits anticancer chemotherapeutic and chemopreventive activities. This compound inhibits development of stomach and oral cancers in vivo and shows some benefit in the treatment of dysplasias. Additionally, this compound induces differentiation…
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GNF-5
Cayman ChemicalA selective allosteric inhibitor of Bcr-Abl (IC50s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…
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Daidzein
Cayman ChemicalAn isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.
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HET0016
Cayman Chemical20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…
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Tetrodotoxin Citrate
Cayman ChemicalA potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.
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ß-Gal-NONOate
Cayman Chemicalβ-Gal-NONOate is a nitric oxide (NO) donor which releases NO following activation by β-galactosidase. β-Gal-NONOate is stabile in aqueous solution at neutral and acidic pH for several hours, exhibits good water solubility, and is able to cross the cell membrane. Following enzymatic…
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11ß-Prostaglandin F1ß
Cayman ChemicalSteroisomer of PGF1α with both C-9 and C-11 hydroxyls inverted.
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3-tert-Butyl-4-Hydroxyanisole
LKT Labs3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…
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Indole-3-Acetic Acid (sodium salt)
Cayman ChemicalA naturally occurring plant hormone of the auxin class that stimulates cell elongation and division, promoting plant growth and development.
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Aflatoxin G1
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G1 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.
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tetranor-PGDM
Cayman ChemicalA major metabolite of PGD2 found in human and mouse urine at levels of approximately 1.5 and 8.1 ng/mg creatinine, respectively.
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Fulvestrant
Cayman ChemicalA potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.
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Vinclozolin M2
Cayman ChemicalA metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).
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KB2115
Cayman ChemicalA synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.
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2-NBDG
Cayman ChemicalA fluorescently-labeled deoxyglucose analog that is used primarily to directly monitor glucose uptake by living cells and tissues; also used as a topical contrast reagent for the detection of neoplasia.
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4-hydroxy Nonenal
Cayman ChemicalA lipid peroxidation product derived from oxidized ω-6 PUFAs such as linoleic acid and arachidonic acid which is widely used as a marker of lipid peroxidation.
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Fura-2 AM
Cayman ChemicalAnoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma
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6-Aminocaproic Acid
LKT Labs6-Aminocaproic acid is a protease inhibitor that displays anticancer activity but is limited by cytotoxicity. 6-Aminocaproic acid inhibits plasmin, preventing fibrinolysis; it may exhibit pro-thrombotic activity, as it is clinically used to treat bleeding disorders.
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1,2-Dimyristoyl-sn-glycero-3-phosphate (sodium salt)
Cayman ChemicalA phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.
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N-Acetyl-S-(N’-phenylthiocarbamoyl)-L-cysteine (PITC) is a cysteine conjugate of N-acetyl-phenylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer…
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8-bromo-Cyclic GMP (sodium salt)
Cayman ChemicalA cell-permeable analog of cGMP that preferentially activates cGMP-dependent protein kinase; 1 µM-0.1 mM inhibits acetylcholine-induced increases in intracellular calcium concentrations.
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RITA
Cayman ChemicalAn inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.
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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.
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ALK5 Inhibitor II
Cayman ChemicalA selective inhibitor of the TGF-β type1 receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…