Bottle, Glass, Clear, Biologically Active Small Molecules
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Nullscript
Cayman ChemicalAn analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.
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Arachidonoyl-1-thio-Glycerol
Cayman ChemicalA thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.
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Rapamycin
Cayman ChemicalAn immunosuppressant used to prevent transplant rejection; potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM); specifically interacts with FKBP12 to form a complex which inhibits mTORC1.
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Vitamin K3
Cayman ChemicalA precursor to Vitamin K2 that is capable of both redox cycling and arylating nucleophilic substrates by Michael addition; used as an antihemorrhagic agent and to inhibit the proliferation of various cancer cells.
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DBZ
Cayman ChemicalA γ-secretase inhibitor that blocks Notch processing (IC50 = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.
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MDV 3100
Cayman ChemicalA non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.
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Doxepin (hydrochloride)
Cayman ChemicalA tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.
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Levofloxacin
Cayman ChemicalA third generation fluoroquinolone with antibacterial activity; inhibits type II topoisomerases (IC50s = 8.06 and 9.81 µg/ml for DNA gyrase and topoisomerase IV, respectively).
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15(R)-HEDE
Cayman Chemical15(R)-HEDE is isolated by the chromatographic resolution of (±)15-HEDE. There are no reports of biological activity associated with 15(R)-HEDE in the literature.
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Eicosapentaenoyl Ethanolamide
Cayman ChemicalAn N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.
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17-AAG
Cayman ChemicalAn analog of geldanamycin which has potent in vivo activity and reduced toxicity; has diverse anti-tumor actions; promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC50 = 4-72 nM).
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ß-Nicotyrine
Cayman ChemicalAn alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.
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5-Fluorouracil
Cayman ChemicalA pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.
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WH-4-023
Cayman ChemicalA selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.
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Unoprostone isopropyl ester
Cayman ChemicalUnoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…
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CFDA-SE
Cayman ChemicalA stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.
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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…
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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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Metformin (hydrochloride)
Cayman ChemicalA biguanide derivative used to lower blood glucose concentrations in patients with non-insulin-dependent diabetes mellitus; 50-400 mg/kg body weight inhibits complex 1 of the mitochondrial respiratory-chain and induces AMP-activated protein kinase-dependent signaling in B6-Lepob/ob mice.
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10-HDA
Cayman ChemicalAn unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…
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Vancomycin (hydrochloride)
Cayman ChemicalA glycopeptide antibiotic identified for its utility in the treatment of gram-positive bacteria, including penicillin-resistant staphylococci; binds to bacterial cell wall precursors, interfering with their synthesis.
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TBTA
Cayman ChemicalA tertiary amine that complexes with, and stabilizes, Cu(I) to accelerate azide-alkyne cycloadditions, as used in click chemistry.
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Acridine Orange
Cayman ChemicalA cell-permeable, fluorescent dye that accumulates in acidic organelles in a pH-dependent manner and is used for autophagy detection and cell cycle determination; emits green fluorescence (ex. max: 502 nm; ,em. max: 525 nm) at neutral pH or when bound to dsDNA and red fluorescence (ex. max: 460 nm;…
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ß-Glycerophosphate (sodium salt hydrate)
Cayman ChemicalA protein phosphatase inhibitor that acts as a phosphate group donor in matrix mineralization studies; 10 mM accelerates calcification of cultured vascular smooth muscle cells through an alkaline phosphatase-related mechanism.
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AFMK
Cayman ChemicalA melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.
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a-Linolenic Acid
Cayman ChemicalALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.
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DL-Sulforaphane N-acetyl-L-cysteine
Cayman ChemicalA major metabolite of sulforaphane that has been shown induce ARE-driven gene expression with roughly 8-fold less potency than sulforaphane.
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Levosimendan
Cayman ChemicalA calcium sensitizer that causes increased cardiac contractility by binding troponin C (EC50 = 9 nM), promotes vasodilation by activating ATP-sensitive potassium channels on vascular smooth muscle cells (EC50 = 0.28 µM), and performs a cardioprotective function by…
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ZD 7288
Cayman ChemicalA potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC50s = 32 and 158 nM, respectively); modulates the sinoatrial node and slows heart rate; reduces neuropathic pain in several animal models.
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GSK2830371
Cayman ChemicalA potent and selective inhibitor of Wip1 (IC50 = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.
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TCPOBOP
Cayman ChemicalAn agonist for mCAR (EC50 = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors; potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.