Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • TPT-260 (hydrochloride)

    Cayman Chemical

    A thiophene thiourea derivative that acts as a chaperone to stabilize the retromer complex against thermal denaturation (Kd = ~5 µM); dose-dependently increases the level of retromer proteins, redirects APP from the endosome, and reduces the formation of pathogenic APP in cultured hippocampal neurons.

  • SB-242084 (hydrochloride)

    Cayman Chemical

    An antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors; brain penetrant with significant anxiolytic activity; used extensively in animal research.

  • 2-NBDG

    Cayman Chemical

    A fluorescently-labeled deoxyglucose analog that is used primarily to directly monitor glucose uptake by living cells and tissues; also used as a topical contrast reagent for the detection of neoplasia.

  • 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.

  • Colcemid

    Cayman Chemical

    A colchicine derivative that inhibits tubulin polymerization (IC50 = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

  • Colistin (sulfate)

    Cayman Chemical

    A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.

  • Ebastine

    Cayman Chemical

    A histamine H1 receptor antagonist (Ki = 0.4 nM; IC50 = 45 nM) that does not cross the blood brain barrier; 10 μM inhibits T cell proliferation and the production of Th2-type pro-inflammatory cytokines by macrophages.

  • Valproic Acid (sodium salt)

    Cayman Chemical

    An analog of valeric acid, long used as an anticonvulsant; inhibits Class I HDACs with an IC50 of ~2 mM; also inhibits GSK3 and depletes cellular IP3.

  • 5-iPF2a-VI

    Cayman Chemical

    Isoprostanes are prostaglandin (PG)-like products of free-radical induced lipid peroxidation. Although the isoprostanes derived from arachidonic acid are the best characterized, many other polyunsaturated fatty acids can form isoprostanes. iPF2α-VI is one of dozens of possible stereo- and…

  • 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.

  • Triptolide

    Cayman Chemical

    The major bioactive constituent of T. wilfordii Hook F., with known antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and antipolycystic kidney disease effects; inhibits human DCTPP1 (Ki = 168 μM; IC50 = 7-10 nM) and COX-2 (IC50 = 0.04 μM).

  • AZD 5363

    Cayman Chemical

    A pan-Akt inhibitor (Akt1, 2, and 3 IC50s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC50s = 6 and 7 nM, respectively) and shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3;…

  • HDAC6 Inhibitor

    Cayman Chemical

    A potent and selective inhibitor of HDAC6 (IC50 = 36 nM) that poorly blocks other HDAC enzymes; cell permeable, inhibiting the acetylation of tubulin in cells with an IC50 value of 210 nM.

  • Coomassie Blue R-250

    Cayman Chemical

    A dye that is commonly used in laboratories to stain or quantify proteins; typically gives blue bands on a clear background with a sensitivity of 50-100 ng/band; displays metachromasia by appearing pink-red, rather than blue, when binding certain proteins, such as collagen and histone H1.

  • Bleomycin (sulfate)

    Cayman Chemical

    A glycopeptide antitumor antibiotic that produces single and double-strand DNA breaks in tumor cells to interrupt their cell cycle; has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models…

  • 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.

  • Xylazine

    Cayman Chemical

    An agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.

  • A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.

  • Olaparib

    Cayman Chemical

    A potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM); can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.

  • Caylin-2

    Cayman Chemical

    A nutlin-3 analog; inhibits the growth of HCT116 cells at high concentrations (IC50 = ~8 µM); promotes the growth of HCT116 cells ~40% at concentrations between 5-100 nM.

  • Kaempferol

    Cayman Chemical

    A dietary flavonoid which has diverse physiological activities through both direct and indirect effects; directly binds ERα and ERβ, acting as an inverse agonist or agonist; acts as an antioxidant; suppresses signaling through certain receptor tyrosine kinases, including EGFR and HGF.

  • 8,12-iso-iPF2a-VI-d11

    Cayman Chemical

    An internal standard for the quantification of 8,12-iso-iPF2α-VI by GC- or LC-MS.

  • 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).

  • HSP-990

    Cayman Chemical

    An Hsp90 inhibitor (IC50s = 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and GRP94, respectively); dissociates the Hsp90-p23 complex, depleting the client protein c-Met and inducing Hsp70 in c-Met amplified GTL-16 gastric tumor cells; inhibits proliferation of various human tumor…

  • AEBSF is a serine protease substrate that inhibits protease activity.

  • Quinolinic Acid

    Cayman Chemical

    An endogenous agonist at NMDA receptors generated through the metabolism of tryptophan in the kynurenine pathway; generates reactive oxygen species, has immunomodulatory actions, and promotes the formation of hyperphosphorylated tau proteins.

  • BMS 833923

    Cayman Chemical

    An orally bioavailable inhibitor of Smo; blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC50s = 6-35 nM); inhibits Shh pathway activity and prevents tumor growth in…

  • A substrate of IMPDH, a NAD+-dependent enzyme that generates xanthosine monophosphate in a rate-limiting step in DNA, RNA, and glycoprotein synthesis; also involved in potentiating the umami taste sensation.

  • DAF-2 diacetate

    Cayman Chemical

    DAF-2 diacetate is a sensitive fluorescent indicator for the detection and bioimaging of NO. It is a cell-permeable derivative of DAF-2. Upon entry into the cell, DAF-2 diacetate is transformed into the less cell-permeable DAF-2 by cellular esterases thus preventing loss of signal due to diffusion…

  • 5-Fluorouracil

    Cayman Chemical

    A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

  • Artesunate

    LKT Labs

    Artesunate is a sesquiterpene lactone derived from Artemisia. Artesunate exhibits anticancer chemotherapeutic, antiviral, anti-angiogenic, and anti-parasitic activities. Artemisinins such as artesunate are best known for their antimalarial activity. Artesunate induces G0/G1 phase cell cycle arrest,…

  • Streptozotocin

    Cayman Chemical

    A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

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