Biologically Active Small Molecules, 100 mg, Cayman Chemical
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1,6-Anhydro-ß-D-mannopyranose
Cayman ChemicalA major organic tracer generated by burned cellulose; used to evaluate, in atmospheric samples, the burning of wood.
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Suberohydroxamic Acid
Cayman ChemicalA competitive HDAC inhibitor that inhibits HDAC1 (IC50 = 0.25 μM) and HDAC3 (IC50 = 0.30 μM); causes cell differentiation, cell cycle arrest, or apoptosis.
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Solifenacin (succinate)
Cayman ChemicalA competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.
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Natamycin
Cayman ChemicalA naturally occurring macrolide polyene used to treat fungal infections, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium (minimal inhibitory concentrations ~ 4-64 μM); also used in the food industry as a "natural" preservative.
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Vandetanib
Cayman ChemicalA broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including VEGFR and EGFR, with IC50 values in the nanomolar range; also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.
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Darifenacin (hydrobromide)
Cayman ChemicalA receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively); effective in treating problems related to the lower urinary tract.
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Salinomycin (sodium salt)
Cayman ChemicalAn antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC50 = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…
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3,4,6-Tri-O-benzyl-ß-D-Mannopyranose 1,2-(methyl orthoacetate)
Cayman ChemicalA synthetic intermediate used in glycosylation reactions.
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Memantine (hydrochloride)
Cayman ChemicalAn NMDA open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties; 12 μM blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity in rat…
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Biocytin
Cayman ChemicalA conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.
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Metolazone
Cayman ChemicalA thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC50 = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).
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N-Palmitoyl Dopamine
Cayman ChemicalA “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…
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DL-Glyceraldehyde-3-phosphate
Cayman ChemicalAn intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.
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Tadalafil
Cayman ChemicalA potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.
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Flumazenil
Cayman ChemicalAn imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC50 = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.
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1-Palmitoyl-2-oleoyl-3-linoleoyl-rac-glycerol
Cayman ChemicalPOL is a common triglyceride component in seed and vegetable oils including olive, sesame, soybean, canola, corn, hazelnut, and many others. POL is one of the standard triglyceride components used for the USP analysis of sesame oil for pharmaceutical applications.
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Isoproterenol (hydrochloride)
Cayman ChemicalA selective β-adrenoceptor agonist that shows high affinity for β1, β2, and β3 (Ki = 224, 458, and 1,570 nM, respectively); inhibits contractions in isolated field stimulated rat vas deferens at low concentrations (EC50 = 45.6 nM); increases cAMP levels and can…
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Camptothecin
Cayman ChemicalA cytotoxic, quinoline alkaloid that inhibits the DNA enzyme topoisomerase I (Top I) by binding the Top1-DNA cleavage complex and inducing DNA-strand breaks; has strong anti-tumor activity and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in…
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Hoechst 33342 (hydrochloride)
Cayman ChemicalA cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.
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(R,S)-Anatabine
Cayman ChemicalA minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.
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N-(p-amylcinnamoyl) Anthranilic Acid
Cayman ChemicalA channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.
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Gestodene
Cayman ChemicalA progesterone analog (i.e., a progestin); does not bind the ER, however, two of its A-ring metabolites can bind ER and possess weak estrogenic activity.
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a-Truxillic Acid
Cayman ChemicalCan be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.
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Temozolomide
Cayman ChemicalAn imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.
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Imatinib (mesylate)
Cayman ChemicalA first generation tyrosine kinase inhibitor that is used in the treatment of CML, GIST, and other cancers; selectively targets certain tyrosine kinases, including c-ABL, PDGFR, KIT, and the oncoprotein BCR-ABL.
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N-(3-hydroxyphenyl)-Arachidonoyl amide
Cayman Chemical3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.
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Pirfenidone
Cayman ChemicalAn orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.
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Omeprazole
Cayman ChemicalA selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).
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ß-Asarone
Cayman ChemicalAmeliorates depression, reduces dopamine-induced neurotoxicity, and attenuates damage in a model of stroke; blocks autophagy, reduces inflammation, and inhibits apoptosis in isolated neurons and in brains; induces apoptosis in colon cancer cells.
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Necrostatin-1
Cayman ChemicalAn inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells with an EC50 value of 490 nM.
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Olmesartan Medoxomil
Cayman ChemicalA prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.