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.

  • 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.

  • Endothall

    Cayman Chemical

    An herbicide that is used to control a wide range of terrestrial and aquatic plants.

  • 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.

  • ß-Glycerophosphate (sodium salt hydrate)

    Cayman Chemical

    A 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.

  • 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.

  • tetrahydro-L-Biopterin (hydrochloride)

    Cayman Chemical

    A required cofactor for many enzymes including all NOS isoforms.

  • 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).

  • 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)…

  • Doxorubicin (hydrochloride)

    Cayman Chemical

    An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

  • 15(R)-Prostaglandin E1

    Cayman Chemical

    15(R)-PGE1 is the “unnatural” C-15 stereoisomer of PGE1. It is essentially inactive biologically when compared to PGE1. It is a non-competitive inhibitor of 15-hydroxy PGDH with an IC50 of 189 µM.

  • 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…

  • 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.

  • 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.

  • Cyclophosphamide (hydrate)

    Cayman Chemical

    A nitrogen mustard alkylating agent used in the treatment of cancers and autoimmune disorders; metabolized to the active compound phosphoramide mustard, which crosslinks with DNA and causes cell death.

  • tetranor-PGDM-d6

    Cayman Chemical

    An internal standard for the quantification of tetranor-PGDM by GC- or LC-MS.

  • Valinomycin

    Cayman Chemical

    A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

  • Glyceryl Triheptadecanoate

    Cayman Chemical

    A saturated triacylglycerol with heptadecanoate (17:0) side-chains attached at the C-1, C-2, and C-3 positions.

  • BIBF 1120

    Cayman Chemical

    A triple receptor tyrosine kinase inhibitor, blocking signaling through VEGFR (IC50 = 13-34 nM), PDGFR (IC50 = 59-65 nM), and FGFR (IC50 = 37-610 nM); inhibits angiogenesis; has potential applications in various forms of cancer and pulmonary fibrosis.

  • Natamycin

    Cayman Chemical

    A 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.

  • Hoechst 33342 (hydrochloride)

    Cayman Chemical

    A 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.

  • (±)-Warfarin

    Cayman Chemical

    A racemic mixture of two optically active isomers, the R and S forms; has a half-life of 36-42 hours in circulation, bound to plasma proteins, and accumulates in the liver, where the two isomers are metabolized by different pathways; also used as a rodenticide.

  • Taurocholic Acid (sodium salt)

    Cayman Chemical

    A bile salt formed in the liver by conjugation of cholic acid with taurine that can be used to solubilize lipids and membrane-bound proteins.

  • 3-Hydroxyglutaric Acid

    Cayman Chemical

    A metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

  • Cyclosporin A

    Cayman Chemical

    An immunosuppressant drug that binds cyclophilin D, inhibiting the phosphatase activity of calcineurin in T cells (IC50 = 5 nM), which interferes with the nuclear import of NFAT, a transcription factor involved in T cell activation; used for the prevention of transplant rejection.

  • DAPI (hydrochloride)

    Cayman Chemical

    A fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications; characterized by ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths.

  • Vildagliptin

    Cayman Chemical

    An inhibitor of DPP-4 (IC50 = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

  • XAV939

    Cayman Chemical

    A small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

  • CHIR99021

    Cayman Chemical

    An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.

  • 11-deoxy Prostaglandin E2

    Cayman Chemical

    11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

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