Biologically Active Small Molecules

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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.

  • ProClin™ 300

    MilliporeSigma

    ProClin biocides are immediately microstatic upon contact with microbial organisms as a result of their ability to quickly penetrate cell membranes and inhibit specific enzymes crucial to cellular respiration. Multiple specific sites of ProClin toxicity prevent microorganisms from developing high…

  • Aflatoxin G1

    Cayman Chemical

    A food contaminant produced by Aspergillus that is associated with toxicity and hepatocarcinogenicity in human and animal populations.

  • 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)…

  • 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.

  • 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.

  • 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…

  • 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).

  • Glyceryl Triheptadecanoate

    Cayman Chemical

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

  • Dihomo-y-Linolenic Acid

    Cayman Chemical

    An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

  • tetranor-PGDM-d6

    Cayman Chemical

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

  • Acarbose

    LKT Labs

    a-Glucosidase inhibitor that decreases digestion of complex carbohydrates and prevents glucose absorption. It improves insulin sensitivity and decreases postprandial hyperglycemia.

  • 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).

  • Curcumin (technical grade)

    Cayman Chemical

    Curcumin is an extract of turmeric root with antioxidant, anti-tumor, and anti-inflammatory properties. Curcumin inhibits the induction of NOS in macrophages.

  • 6-diazo-5-oxo-L-nor-Leucine

    Cayman Chemical

    A glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.

  • Ursolic Acid

    Cayman Chemical

    A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

  • Rhodamine 110 (chloride)

    Cayman Chemical

    A green fluorescent cationic dye (ex/em max 496/520 nm) that is incorporated with a hydrolytic substrate (e.g., proteinase or peptidase substrates) for use as a highly sensitive detection reagent in fluorescence-based enzyme assays.

  • JC-1

    Cayman Chemical

    A membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis; changes fluorescence characteristics with alteration in mitochondrial transmembrane potential, a very early event in apoptosis.

  • Gossypol

    Cayman Chemical

    A racemic mixture of natural polyphenols that inhibits spermatogenesis; has antimalarial properties, preventing the growth of P. falciparum; inhibits aldose reductase (Ki = 0.5 µM); inhibits growth in various cancer cell lines at low micromolar concentrations.

  • Cytochalasin E

    Cayman Chemical

    Inhibits actin polymerization; potently and selectively inhibits the growth of endothelial cells (IC50 1 protease activity.

  • Ciprofloxacin

    LKT Labs

    Ciprofloxacin is a second generation fluoroquinolone antibiotic that exhibits antibacterial activity against both gram negative and gram positive bacteria. Ciprofloxacin inhibits DNA gyrase and topoisomerase IV, preventing DNA replication.

  • Calcein AM

    Cayman Chemical

    A cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.

  • Rifampicin

    Cayman Chemical

    A member of the rifamycin class of antibiotics, inhibiting bacterial DNA-dependent RNA synthesis (Ki = ~ 1 nM); activates PXR (EC50 = ~2 µM), up-regulating enzymes that alter drug metabolism; inhibits OATPs with Ki/IC50 values ranging from 0.58-18 µM.

  • 3'-Azido-3'-deoxythymidine

    LKT Labs

    AZT is a thymidine nucleoside analog that inhibits reverse transcriptase and is clinically used to treat HIV/AIDS. AZT inhibits viral DNA synthesis, preventing viral replication; at high doses, it may inhibit DNA polymerase. Use of AZT is often limited

  • Ceftriaxone Sodium

    LKT Labs

    Ceftriaxone is a third generation β-lactam cephalosporin antibiotic. Ceftriaxone exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding protein activity to prevent peptidoglycan synthesis and bacterial cell wall formation. Ceftriaxone is…

  • Colchicine

    Cayman Chemical

    Inhibits microtubule polymerization (IC50 =3.2 μM) by binding to tubulin, which disrupts spindle formation during mitosis; blocks the growth of MCF-7 human breast carcinoma cells (IC50 = 13 nM); inhibits neutrophil motility and activity (5 μmol/kg in a mouse model of…

  • Coenzyme Q1

    Cayman Chemical

    An amphipathic CoQ10 homolog that has a tail consisting of five isoprene units. It has been used as an electron acceptor to study a range of oxidoreductases as isolated enzymes, in subcellular fractions, in intact cells in culture, and in perfused organs.

  • UCN-02

    Cayman Chemical

    A PKC inhibitor (IC50 = 62 nM) that is cytotoxic to the growth of HeLa S3 cells.

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