Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • GSK5959

    Cayman Chemical

    A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

  • 10-POHSA

    Cayman Chemical

    A FAHFA in which palmitoleic acid is esterified to 10-hydroxy stearic acid.

  • Leukotriene B4-3-aminopropylamide

    Cayman Chemical

    An analog of LTB4 that binds to the BLT1 and BLT2 receptors with Ki values of 5.1 and 1,227 nM, respectively.

  • Ispinesib

    Cayman Chemical

    The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells. Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM)…

  • DG-172 (hydrochloride)

    Cayman Chemical

    An orally available inverse agonist of PPARβ/δ (IC50 = 27 nM), down-regulating transcription of ANGPTL4 in mouse myoblasts (IC50 = 9.5 nM).

  • REV 5901

    Cayman Chemical

    REV 5901 is an antagonist of cysteinyl-leukotriene receptors with a Ki value of 0.7 µM for guinea pig lung membranes. It is also an inhibitor of rat neutrophil 5-LO with an IC50 value of 0.12 µM.

  • N-(2-hydroxyethyl)-Naphthalimide

    Cayman Chemical

    An N-substituted 1,8-naphthalimide used as a fluorescent probe for various studies and as a precursor for protection of amine groups.

  • GW 9578

    Cayman Chemical

    A potent, selective PPARα agonist that activates murine and human PPARα with EC50 values of 0.005 and 0.05 µM, respectively; 0.2 mg/kg given orally once daily for three days decreased serum total LDL cholesterol 40-60% in male Sprague-Dawely rats.

  • (R,S)-Anatabine

    Cayman Chemical

    A 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.

  • Acetaminophen

    Cayman Chemical

    An analgesic and antipyretic compound; inhibits COX-2 activity by more than 80%, albeit at relatively high doses, while it is less effective against COX-1.

  • Vancomycin (hydrochloride)

    Cayman Chemical

    A 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.

  • Melatonin

    Cayman Chemical

    An indoleamine neurohormone whose levels vary in a daily cycle, thereby allowing the entrainment of the circadian rhythms of several biological functions in animals, plants, and microbes; acts as a powerful antioxidant that protects lipids, proteins, and DNA against oxidative damage.

  • Thiostrepton

    Cayman Chemical

    A natural peptide thiazole antibiotic that inhibits FoxM1 in mammalian cells, preventing the expression of FoxM1-regulated genes; prevents proliferation and induces apoptosis in human cancer cells; also acts as a proteasome inhibitor.

  • 1-Deoxynojirimycin (hydrochloride)

    Cayman Chemical

    A glucose analog that potently inhibits α-glucosidase I and II to prevent the formation of complex N-linked oligosaccharides (IC50= ~2 µM).

  • 2-amino-4-phenyl Thiazole

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • Capsaicin (technical grade)

    Cayman Chemical

    Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…

  • Carbetapentane (citrate)

    Cayman Chemical

    An agonist of the sigma-1 receptor (Ki = 10.4 nM); also binds the serotonin 5-HT3 and muscarinic acetylcholine receptors (Kis = 7.9 and 76 nM, respectively).

  • 2-Amino-5-fluorobenzoic Acid

    Cayman Chemical

    A toxic antimetabolite for the tryptophan pathway in yeast that can be used to counterselect for TRP1, a commonly used genetic marker in S. cerevisiae.

  • SC-1

    Cayman Chemical

    A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.

  • Ibotenic Acid

    Cayman Chemical

    A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

  • Inauhzin

    Cayman Chemical

    A cell-permeable, selective SIRT1 inhibitor (IC50 = 0.7-2 µM) that reactivates p53 by inhibiting SIRT1 deacetylation activity; inhibits cell proliferation by inducing p53-dependent apoptosis in various human cancer cells (IC50s = 5.4, 51.9, 3.2, 33.9, and 85.4 µM…

  • Pioglitazone (potassium salt)

    Cayman Chemical

    Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands. Pioglitazone is a closely related TZD which also…

  • Amylose

    Cayman Chemical

    A polysaccharide made of α-D-glucose units that constitutes about 20% of starch; acts as an indicator, turning blue in the presence of iodine, and has also been coupled to magnetic beads for the isolation and purification of maltose-binding protein fusion proteins.

  • (E/Z)-4-hydroxy Tamoxifen

    Cayman Chemical

    An active metabolite of tamoxifen that is formed by the action of CYP2D6 in human liver; inhibits MCF-7 and MDA-MB 231 cell proliferation with IC50 values of 27 and 18 µM, respectively; stimulates LC3 lipidation and formation of autophagic vesicles.

  • HDMAPP (ammonium salt)

    Cayman Chemical

    A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

  • Trolox

    Cayman Chemical

    A cell-permeable, water-soluble derivative of vitamin E with potent antioxidant properties; commonly used as a standard or positive control in antioxidant assays.

  • WSP-1

    Cayman Chemical

    A reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells.

  • PF-04691502

    Cayman Chemical

    A potent, dual inhibitor of PI3K and mTOR that selectively inhibits human PI3K isoforms α, β, δ, and γ (Kis = 1.8, 2.1, 1.6, and 1.9 nM, respectively) and human mTOR (Ki = 16 nM).

  • D-Luciferin (potassium salt)

    Cayman Chemical

    A chemiluminescent substrate of firefly luciferase which produces light upon oxidative decarboxylation in the presence of ATP.

  • Capsaicin

    Cayman Chemical

    The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

  • MK-0457

    Cayman Chemical

    A potent pan-Aurora kinase inhibitor that favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM); inhibits proliferation of clear cell renal carcinoma (IC50 = 2/M phase.

  • Tenovin-1

    Cayman Chemical

    A small molecule activator of p53 that decreases the growth of BL2 Burkitt’s lymphoma and ARN8 melanoma cells; inhibits the deacetylase activity of purified human SIRT1 and SIRT2.

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