Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • BYL719

    Cayman Chemical

    A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

  • Guanylyl Imidodiphosphate

    Cayman Chemical

    A nonhydrolyzable GTP analog that binds to and irreversibly activates G proteins; potently stimulates adenylate cyclase.

  • Okadaic Acid

    Cayman Chemical

    A potent inhibitor of certain serine/threonine protein phosphatases, targeting the multiple isoforms of PP1 (IC50 = 10-50 nM), both isoforms of PP2A (IC50 = 0.5 nM) and PP3 (IC50 = 4 nM); a very weak inhibitor of PP2B (IC50 > 2 μM); does not inhibit PP2C or other phosphatases.

  • FTY720 Phosphate

    Cayman Chemical

    A potent agonist at four of the sphingosine-1-phosphate (S1P) receptors with IC50 values of 0.2-6 nM.

  • Oleanolic Acid

    Cayman Chemical

    A triterpenoid with anti-inflammatory, anti-hyperlipidemic, and hepatoprotective in vivo effects; also has antiviral and anti-tumor actions; binds specific proteins, altering their activity.

  • LH 846

    Cayman Chemical

    LH 846 is a benzothiazole analog that selectively inhibits casein kinase (CK) 1δ (IC50 = 290 nM). It inhibits CK1ε and CK1α at much higher concentrations (IC50s = 1.3 and 2.5 μM, respectively) but does not inhibit CK2. LH 846 has been shown to inhibit…

  • IWR-1-exo

    Cayman Chemical

    An ideal control for the inhibitor of Wnt response compound, IWR-1-endo.

  • 3-Methyladenine

    Cayman Chemical

    A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

  • PKC? Pseudosubstrate Inhibitor

    Cayman Chemical

    A synthetic peptide that that selectively, reversibly, and substrate-competitively inhibits PKCζ activity and, thus, is used to delineate the signaling functions of PKCζ.

  • PKCe Inhibitor Peptide

    Cayman Chemical

    A synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC?; selectively and reversibly inhibits the translocation of PKC? to intracellular membranes, blocking activation.

  • (1S,3R)-3-Hydroxycyclopentane acetic acid

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • FBBBE

    Cayman Chemical

    A derivatized fluorescein compound that is used to detect the production H2O2 by cells; converted to fluorescein by intracellular H2O2, resulting in an increase in intracellular fluorescence (excitation/emission maxima: 480/512 nm).

  • (±)12-HpETE

    Cayman Chemical

    (±)12-HpETE is one of the six monohydroperoxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid (Item No. 90010) and consists of an equal mixture of the R and S isomers. Reduction of the hydroperoxide yields the more stable hydroxyl fatty acid (±)12-HETE (Item…

  • AFMK

    Cayman Chemical

    A 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.

  • 2-Aminopurine (hydrochloride)

    Cayman Chemical

    A fluorescent analog of guanosine and adenosine that is used as a site-specific probe of nucleic acid structure and dynamics, such as studies of base stacking interactions and DNA base flipping; inhibits PKR.

  • 4-formyl Indole

    Cayman Chemical

    Indole-4-carboxaldehyde is a synthetic intermediate useful for pharmaceutical synthesis.

  • Tolterodine (tartrate)

    Cayman Chemical

    A competitive antagonist of muscarinic (M) receptors (Ki = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1 through M5, respectively).

  • 4,5-dehydro Docosahexaenoic Acid

    Cayman Chemical

    A novel analog of DHA in which the double bond closest to the carboxyl group has been substituted with a triple bond; the corresponding acetylene in arachidonic acid is a well known inhibitor of 5-LO.

  • 13,14-dihydro-15-keto Prostaglandin D1

    Cayman Chemical

    A theoretical metabolite of PGD1.

  • 6ß-Prostaglandin I1

    Cayman Chemical

    6β-PGI1 is a stable PGI2 analog resistant to hydrolysis in aqueous solutions. 6β-PGI1 has a much longer half-life than PGI2, but a greatly reduced molar potency for receptor mediated function. 6β-PGI1 has a Kact for adenylate cyclase in NCB-20 cells of 4.2 µM compared with 18…

  • VU0255035

    Cayman Chemical

    A selective, competitive orthosteric antagonist of the muscarinic M1 receptor (IC50 = 130 nM); is effective in cells and in vivo and brain penetrating, blocking pilocarpine-induced seizures without disrupting contextual fear conditioning in mice.

  • R406

    Cayman Chemical

    A potent orally available inhibitor of Syk (Ki = 30 nM); blocks FcεRI-dependent mast cell activation (EC50 = 43 nM) and, at 3 μM, reduces the release of IL-10, -12, and -13 by immune complex-pulsed dendritic cells.

  • 1,2-Dioctanoyl-sn-glycerol

    Cayman Chemical

    A cell permeable analog of the PKC-activating second messenger DAG.

  • D-myo-Inositol-1,2-diphosphate (sodium salt)

    Cayman Chemical

    A member of the InsP family of small, soluble second messengers.

  • Arachidonyl Trifluoromethyl Ketone

    Cayman Chemical

    ATK is an analog of arachidonic acid in which the carboxyl group is replaced by a trifluoromethyl ketone group. It inhibits the activity of the 85 kDa cPLA2 and the 80 kDa macrophage iPLA2 without altering the activity of the 14 kDa sPLA2s. ATK is useful for differentiating the effects of cPLA2 and…

  • CAY10719

    Cayman Chemical

    A selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 µM).

  • RSC-133

    Cayman Chemical

    Promotes the reprogramming of human somatic cells to pluripotent stem cells; increases the number of human foreskin fibroblasts that express alkaline phosphatase when used at 10 μM with four standard reprogramming factors; down-regulates inducers of cellular senescence and inhibits Dnmt1 and HDAC1.

  • ThioFluor 623

    Cayman Chemical

    Reacts with thiols resulting in an increase in fluorescence intensity of up to 120-fold; the response is selective for thiols, occurs in aqueous media, and results in a fluorophore with emission at 623 nm; cell-permeable.

  • PtdIns-(4)-P1 (1,2-dipalmitoyl) (ammonium salt)

    Cayman Chemical

    A synthetic analog of natural PtdIns featuring C16:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

  • Amphotericin B

    Cayman Chemical

    A polyene macrolide used in the treatment of infections caused by C. albicans, A. fumigatus, and parasitic L. protozoans, as well as in tissue culture to prevent fungi from contaminating cell cultures; binds with ergosterol in fungal cell membranes, altering membrane permeability and ultimately…

  • Uridine-3'-monophosphate (sodium salt)

    Cayman Chemical

    A nucleoside used in the biochemical synthesis of ribothymidine-3’-phosphate that has been used as a bioavailable source of uridine in research studies designed to enhance learning and memory.

  • 1,2,3,4,6-Penta-O-galloyl-ß-D-glucopyranose

    Cayman Chemical

    A major component of the root of P. suffruiticosa that at 30 µM inhibits the growth of human hepatocellular carcinoma SK-HEP-1 cells by causing cell cycle arrest and suppressing the activation of NF-κB.

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