Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Dalcetrapib

    Cayman Chemical

    An inhibitor of CETP; inhibits plasma CETP with an IC50 value of 9 µM; in rabbits given an atherogenic diet, increases HDL, decreases VLDL, and attenuates induced atherosclerosis; in humans, inhibits CETP activity and increases HDL levels but does not reduce the risk of recurrent…

  • Chlorpheniramine is a first generation alkylamine antihistamine that inhibits H1 histamine receptors, serotonin transporters (SERT), and norepinephrine transporters (NET); it exhibits anti-allergic and antidepressant activities. Chlorpheniramine is clinically used to treat allergic rhinitis and…

  • Biotin-azide

    Cayman Chemical

    A form of biotin with a terminal azide group; is used to add biotin to other molecules that bear either an alkyne group, through click chemistry, or a phosphine group, using Staudinger ligation.

  • S-Adenosylhomocysteine

    Cayman Chemical

    An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

  • A potent inhibitor of PDE5 (IC50 = 0.2-1.2 nM) that less effectively blocks the activities of PDE6, PDE1, and PDE11 (IC50s = 2, 230, and 130 nM, respectively).

  • Abacavir

    LKT Labs

    Guanosine analog and inhibitor of RT, guanylyl cyclase, and telomerase used to treat HIV infection.

  • OXA-01

    Cayman Chemical

    A selective dual inhibitor of mTORC1 and mTORC2.

  • SC-514

    Cayman Chemical

    A selective and reversible inhibitor of IKK2 (IC50 = 3- 12 μM) that displays >10-fold selectivity over 28 other kinases; attenuates NF-κB-mediated gene expression in synovial fibroblasts, smooth muscle cells, and astrocytes.

  • 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…

  • Norethindrone

    MP Biomedicals

    Norethindrone is a synthetic progestin that possesses antiestrogenic effects, where in low doses it is progestational and in high doses it is antiestrogenic. It also causes a time-dependent loss of cytochrome P-450 when incubated in vitro with rat liver microsomal fractions and NADPH-generating…

  • A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

  • Arachidonoyl p-Nitroaniline

    Cayman Chemical

    ApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…

  • PAF C-16 Carboxylic Acid

    Cayman Chemical

    Modified with a carboxylic acid group terminating the C-16 alkyl chain, providing a convenient site for chemical crosslinking.

  • WYE-354

    Cayman Chemical

    A selective, potent, and cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

  • 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.

  • Tetrazolium (chloride)

    Cayman Chemical

    A redox indicator used to detect cellular respiration; primarily reduced by Complex I in mitochondria and, under anaerobic conditions, is completely reduced to an insoluble red 1,3,5-triphenylformazan.

  • Cantharidin

    LKT Labs

    Canthardin is a toxin initially produced by the blister beetle, Canarthis vesicatoria. Canthardin competitively inhibits serine/threonine phosphatases such as protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A). Canthardin exhibits anticancer and anti-resorptive activities. In cancer…

  • N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-4AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.1 and 0.625 µM, respectively. It is about 80 times less potent as an inhibitor of…

  • 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.

  • Bilirubin is the principal pigment of bile and constituent of many biliary calculi and also found in blood. As the major end-product of the biological breakdown of heme, bilirubin is the chromophore responsible for coloration in various forms of jaundice. Bilirubin is suitable for use in the…

  • Produced from Ins(1,2,3,5,6)P5 via a minor enzymatic phytate degradation pathway by K. terrigena; moderately effective in opening calcium channels relative to Ins(1,4,5)P3.

  • Diethylstilbestrol

    Cayman Chemical

    Diethylstilbestrol (DES) is a synthetic estrogen receptor agonist that was prescribed to pregnant women in the late 1930s. It was banned in 1971 because of possible links to increased risk of breast cancer in mothers along with congenital abnormalities and increased risk of cancer in offspring. DES…

  • Resazurin (sodium salt)

    Cayman Chemical

    A blue non-fluorescent dye that is used as an oxidation-reduction indicator in cell viability assays in a variety of cells; can be reduced to the highly red-fluorescent product resorufin (excitation: 530-540 nm; emission: 585-595 nm) and used as a quantifiable detection agent in enzyme activity or…

  • EGTA AM

    Cayman Chemical

    A cell-permeant acetoxymethyl ester of the calcium chelator EGTA.

  • Naringenin

    Cayman Chemical

    A citrus-derived flavonoid that inhibits CYP3A4 activity in human liver microsomes (IC50s = 139-188 μM); demonstrates antifibrotic, lipid lowering, and insulin-like properties.

  • Sodium acetate stock solution (3 M, pH 5.2) contains a concentrated solution of filtered sodium acetate buffer.

  • 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.

  • 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.

  • This mixture contains the primary COX products produced by most mammalian tissues. Contents: Prostaglandin D2, Prostaglandin E2, 6-keto Prostaglandin F1α, Prostaglandin F2α, and Thromboxane B2 (100 µg each).

  • Capsaicin is an agonist of transient receptor potential vanilloid (TRPV) channels that was originally found in peppers of the Capsicum genus. Capsaicin exhibits analgesic, anti-inflammatory, anti-obesity, and anticancer chemotherapeutic activity. Capsaicin also displays bronchoconstrictive activity…

  • Sulindac sulfone

    Cayman Chemical

    An oxidized metabolite of sulindac that is produced in many mammals but minimally in mice and rats; generally considered to be inactive against COX enzymes, although it can reduce azoxymethane-induced colon cancer in rats; inhibits aldose reductase (IC50 = 367 nM) in vitro.

  • T0070907

    Cayman Chemical

    A potent and selective PPARγ antagonist with an apparent IC50 value of 1 nM for the human receptor.

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