Biologically Active Small Molecules, Chemicals
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Tianeptine (sodium salt)
Cayman ChemicalAn atypical antidepressant with diverse actions, most notably on the glutamatergic system; attenuates glutamate release and modulates the function of AMPAR; acts as an agonist of the µ-opioid receptor (EC50s = 194 and 641 nM for human and mouse receptors, respectively).
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YS-035 (hydrochloride)
Cayman ChemicalA verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.
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CK-636
Cayman ChemicalA cell-permeable inhibitor of Arp2/3 complex action that inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC50s = 4, 32, and 24 µM, respectively); prevents the formation of actin filament comet tails by Listeria in infected SKOV3 cells…
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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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Albendazole
LKT LabsAlbendazole is a benzimidazole compound that exhibits anti-parasitic and anticancer chemotherapeutic activities. Albendazole displays anti-helminthic benefit in the treatment of worm infections in humans and animals. Albendazole also displays antimitotic properties, binding the colchicine site of…
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SB 277011A (hydrochloride)
Cayman ChemicalA selective antagonist of the dopamine D3 receptor (pKi = 8.0); has high oral bioavailability and enters the central nervous system of the rat.
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trans-Resveratrol-d4
Cayman ChemicalAn internal standard for the quantification of trans-resveratrol by GC- or LC-MS.
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FH535
Cayman ChemicalAn inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ; blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ; selectively toxic to some carcinoma cell lines expressing the…
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Pinostilbene
Cayman ChemicalA stable, monomethoxylated resveratrol derivative that at 0.1-10 μM reduces neurotoxicity in SH-SY5Y cells induced by the parkinsonian mimetic 6-OHDA and scavenges DPPH radicals (IC50 = 47.1 μM).
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Trolox
Cayman ChemicalA cell-permeable, water-soluble derivative of vitamin E with potent antioxidant properties; commonly used as a standard or positive control in antioxidant assays.
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NQDI-1
Cayman ChemicalA selective inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.
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Harringtonine
Cayman ChemicalA natural alkaloid that inhibits protein synthesis at low micromolar concentrations; immobilizes ribosomes immediately after the initiation of translation.
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all-trans Retinal
Cayman ChemicalA natural retinoid that associates with CRBP-I and CRBP-II (Kds = 50 and 90 nM, respectively), which are involved in the intracellular transport of retinol; an intermediate of the phototransduction pathway of photoreceptors; can form toxic conjugates with proteins and lipids, leading to…
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Y-27632 (hydrochloride)
Cayman ChemicalA potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.
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?12-Prostaglandin D2
Cayman ChemicalPGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…
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Diallyl Trisulfide
Cayman ChemicalAn organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…
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Licofelone
Cayman ChemicalA dual inhibitor of COX and LOX pathways, that decreases levels of PGE2, LTB4, and lipoxins and prevents LPS-stimulated IL-1β expression.
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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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AAL-993
Cayman ChemicalA potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively; orally bioavailable in vivo, blocking VEGF-induced angiogenesis and preventing the growth of primary tumors and spontaneous peripheral metastases in mice.
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(-)-Bilobalide
LKT LabsBilobalide is a sesquiterpene lactone found in Ginkgo that exhibits neuroprotective, cognition enhancing, anxiolytic, antioxidative, anti-inflammatory, and analgesic activities. Bilobalide inhibits GABA-A receptors, decreases anxiety, and improves spatial learning and memory in vivo. In animal…
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VER-49009
Cayman ChemicalAn Hsp90 inhibitor with an IC50 value of 47 nM; induces the expression of HSP27 and Hsp72 while reducing the client proteins c-Raf, B-Raf, survivin, and PRMT5, causing cell cycle arrest and apoptosis.
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Normal Goat Serum
Cayman ChemicalThis solution can be used (without further dilution) as a blocking agent for immunocytochemistry or immunohistochemistry when using a secondary antibody generated in goat.
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Floxuridine
Cayman ChemicalA prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC50 = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.
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15(S)-15-methyl Prostaglandin F2a methyl ester
Cayman Chemical15(S)-15-methyl PGF2α methyl ester is a derivative of 15(S)-15-methyl PGF2α with increased membrane permeability. Hydrolysis of the methyl ester in vivo releases the biologically active 15(S)-15-methyl PGF2α, which is a potent uterine stimulant and abortifacient.
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8-CPT-Cyclic AMP (sodium salt)
Cayman ChemicalA lipophilic activator of PKA and PKG (Ka = 0.05 and 0.11 μM, respectively); inhibits PDE VA, PDE III, and PDE IV with IC50 values of 0.9, 24, and 25 μM, respectively.
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ON-01910 (sodium salt)
Cayman ChemicalA potent, non-ATP-competitive inhibitor of Plk1 (IC50 = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.
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Zanamivir
Cayman ChemicalA sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles; selectively inhibits the growth of influenza A and B viruses in plaque reduction assays (IC50s = 5-14 nM) and to directly inhibit influenza A and B virus neuraminidases…
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AZ 20
Cayman ChemicalA potent, selective inhibitor of ATR (IC50 = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.
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N-Arachidonoyl-L-Serine
Cayman ChemicalAn endocannabinoid analog that does not bind to CB1, CB2, or TRPV1; at 5 mg/kg antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model; relaxes isolated rat mesenteric arteries and abdominal aorta, and increases the…
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Amitriptyline Hydrochloride
LKT LabsAmitriptyline exhibits antidepressant, antipsychotic, analgesic, and antinociceptive activities; it acts as an antagonist at 5-HT2A/2C/6/7 receptors, M1-5 muscarinic acetylcholine receptors (mAChRs), H1/4 histamine receptors, a1-adrenergic receptors, and also on the serotonin transporter (SERT) and…
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