Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • 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.

  • Norgestrel

    Cayman Chemical

    A progestin that is a racemic mixture of which levonorgestrel is the biologically active component.

  • AS-1892802

    Cayman Chemical

    Formal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C20H19N3O2

  • 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.

  • Pterostilbene

    Cayman Chemical

    A naturally-occurring dimethyl ether analog of resveratrol; acts as a powerful antioxidant, suppresses the synthesis of PGE2 from LPS-stimulated human peripheral blood mononuclear cells (IC50 = 1.0 μM), and inhibits cell proliferation (IC50 = ~60 μM); evokes effects that…

  • Sclerotiorin

    Cayman Chemical

    A natural product that inhibits soybean LO-1 (IC50 = 4.2 µM), cholesterol ester transfer protein (IC50 = 19.4 µM), Grb2-Shc interaction (IC50 = 22 µM), and antagonizes endothelin receptors (IC50 = 114 and 152 µM for human ETA and…

  • 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.

  • Ibuprofen

    Cayman Chemical

    A non-selective, reversible COX inhibitor. with IC50 values for human recombinant COX-1 and -2 at 2.6 and 1.53 µM, respectively; Ki values for ovine COX-1 and -2 are both 9 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…

  • 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.

  • HAMI3379

    Cayman Chemical

    A potent, selective CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 37.9 and >10, 000 nM, respectively.

  • Echinomycin

    Cayman Chemical

    A cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the HRE; reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50…

  • Tauroursodeoxycholic Acid

    Cayman Chemical

    A secondary bile acid with hepatoprotective properties; inhibits apoptosis, in part by interfering with the mitochondrial pathway of cell death, inhibiting ROS, reducing ER stress, and stabilizing the unfolded protein response.

  • tetranor-PGDM-d6

    Cayman Chemical

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

  • Triphenylphosphine oxide

    Cayman Chemical

    A coordinating solvent used to activate crystallization of chemical compounds; used in flame retardant applications, as an epoxy cure catalyst, and to produce nanostructures.

  • 10-POHSA

    Cayman Chemical

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

  • Bromelain

    Cayman Chemical

    A mixture of proteolytic enzymes derived from the stem and fruit of pineapple plants; studied for a number of potential beneficial effects including anti-inflammatory, anti-thrombotic, fibrinolytic, and anti-cancer functions.

  • ZLN005

    Cayman Chemical

    A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

  • Biliverdin (hydrochloride)

    Cayman Chemical

    A green bile pigment produced from the oxidation of heme in a reaction catalyzed by heme oxygenase and further reduced to bilirubin by biliverdin reductase; possesses anti-mutagenic and antioxidant properties, scavenging free radicals.

  • Inulin

    Cayman Chemical

    A naturally produced dietary fiber that is sometimes categorized as a prebiotic; used to measure kidney function by determining the glomerular filtration rate.

  • 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.

  • NVP-BSK805 (hydrochloride)

    Cayman Chemical

    A potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM); orally bioavailable with a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice.

  • 8,12-iso-iPF2a-VI

    Cayman Chemical

    The most abundant isoprostane product formed during lipid peroxidation; detected after CCl4-induced oxidative damage to hepatic tissue and has been found elevated in the urine, blood, and CSF of patients with Alzheimer’s disease.

  • Prostaglandin I2 (sodium salt)

    Cayman Chemical

    PGI2 is an unstable COX metabolite detected first in vascular endothelial cells. It elevates platelet cAMP and is a potent vasodilator and inhibitor of human platelet aggregation with an IC50 value of 5 nM. PGI2 is stable in basic buffers (pH=8), but it is rapidly hydrolyzed to 6-keto…

  • 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).

  • Disulfiram

    Cayman Chemical

    A copper and zinc chelator and an irreversible inhibitor of aldehyde dehydrogenase (IC50 = 0.1 mM) that has been indicated for the treatment of alcohol dependence; targets the ubiquitin-proteasome pathway, induces ROS, activates JNK and p38 pathways, and inhibits NF-κB activity in…

  • 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…

  • 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.

  • Pentylenetetrazole

    Cayman Chemical

    A central nervous system modulator that is used to experimentally induce seizures in animals; used extensively to screen for compounds that block the production of nonconvulsive (absence or myoclonic) seizures.

  • Bromophenol Blue

    Cayman Chemical

    Commonly used as a pH indicator, a color marker in agarose or polyacrylamide gel electrophoresis, and a dye to detect proteins and nucleic acids (absorbance at 610 nm), particularly when staining living tissues.

  • Latrunculin A

    Cayman Chemical

    A bioactive macrolide derived from sponges that binds monomeric actin, preventing actin polymerization both in vitro (Kd = 0.2 μM) and in cells (0.5 μM).

  • Syk Inhibitor II (hydrochloride)

    Cayman Chemical

    A cell-permeable, selective, and reversible inhibitor of Syk (IC50 = 41 nM); prevents FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and inhibits passive cutaneous anaphylaxis reactions in mice (ID50 = 13.2 mg/kg, s.c.).

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