Biologically Active Small Molecules, 100 mg
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Gly-Phe-ß-naphthylamide
Cayman ChemicalA substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.
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L-Leucine 4-methoxy-ß-naphthylamide (hydrochloride)
Cayman ChemicalA cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.
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PDM 11
Cayman ChemicalA structural analog of several resveratrol derivatives which act as a potent and selective AhR antagonists and agonist.
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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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Montelukast (sodium salt)
Cayman ChemicalThe CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…
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7-Piperazin-1-yl-thieno[2,3-c] Pyridine (hydrochloride)
Cayman Chemical7-Piperazin-1-yl-thieno[2,3-c] pyridine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.
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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.
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Irbesartan
Cayman ChemicalAn angiotensin II receptor blocker with a high affinity for the AT1 receptor (Ki = 2.7 nM) and exceptionally high bioavailability (60-80%); an insurmountable antagonist of AT1; act as a cardiovascular protective agent by effectively reducing blood pressure; also useful in treating diabetes and…
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25-hydroxy Cholesterol
Cayman ChemicalA side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of SREBPs; has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor and immunomodulating activities.
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Doripenem
Cayman ChemicalA broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.
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Ganciclovir
Cayman ChemicalA synthetic analog of 2'-deoxy-guanosine which is used to treat or prevent cytomegalovirus (CMV) infections; inhibits the replication of human CMV with an IC50 value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.
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Fluvoxamine (maleate)
Cayman ChemicalA selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.
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3-Methyladenine
Cayman ChemicalA specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.
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Nocodazole
Cayman ChemicalReversibly binds tubulin and alters GTP hydrolysis as well as microtubule dynamics; nanomolar concentrations reduce both microtubule elongation and shortening velocities, resulting in arrest of cycling in a G2/M phase; also used to induce the formation of Golgi ministacks in eukaryotic cells.
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Gaboxadol (hydrochloride)
Cayman ChemicalA GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist…
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Imiquimod
Cayman ChemicalAn imidazoquinoline compound that activates TLR7 (EC50 = 2.1 µM) on immune cells, inducing the production of IFN-α, IL-12, and other mediators; up-regulates the OGF receptor on cancer cells, blocking cell proliferation (IC50 = 2 µM).
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GYY 4137
Cayman ChemicalA water-soluble, slow-releasing H2S donor which demonstrates vasodilator and anti-hypertensive activity in hypertensive rats when given intravenously; also protects against endotoxic shock in rats, inhibiting pro-inflammatory signaling.
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Clenbuterol (hydrochloride)
Cayman ChemicalA sympathomimetic β2-adrenoceptor agonist that relaxes bronchial smooth muscle and at higher doses acts as an anabolic steroid, promoting skeletal muscle protein synthesis.
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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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Norgestrel
Cayman ChemicalA progestin that is a racemic mixture of which levonorgestrel is the biologically active component.
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2,3-bis (4-Hydroxyphenyl) Propionitrile
Cayman ChemicalAn ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.
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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.
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RG-108
Cayman ChemicalA non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.
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Doxazosin (mesylate)
Cayman ChemicalA non-selective α-adrenergic receptor antagonist with pKi values of 8.5, 9, and 8.4 for human α1A, α1B, and α1D adrenoceptors, respectively; used to relax smooth muscles of the prostate in clinical studies designed to examine treatments that improve lower urinary tract…
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Concanavalin A
Cayman ChemicalA plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…
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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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Cisplatin
LKT LabsCisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…
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Bosutinib
Cayman ChemicalBest known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively); can be effective in regulating tumor growth and differentiation; also inhibits other members of the Src and TEC families and certain other kinases at nanomolar concentrations.
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Melatonin
MP BiomedicalsMelatonin is a hormone of the pineal gland. Hormone; mediates photoperiodicity in mammals; inhibits cerebellar nitric oxide synthetase; peroxynitrite scavenger. Melatonin has complex effects on apoptotic pathways, inhibiting apoptosis in immune cells and neurons but enhancing apoptotic cell…
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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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17-Octadecynoic Acid
Cayman ChemicalA suicide inhibitor of LTB4 20-hydroxylase and renal CYP450 ω-hydroxylase.
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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…