Biologically Active Small Molecules

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Cayman Chemical 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.

  • HA-14-1

    Cayman Chemical

    A small molecule inhibitor of Bcl-2 proteins (IC50 = ~ 9 µM) that induces apoptosis of human acute myeloid leukemia (HL-60) cells (50 µM induces 90% loss of viability).

  • Tranexamic Acid

    Cayman Chemical

    An inhibitor of fibrinolysis that blocks the interaction of plasmin with fibrin (IC50 = 3.1 µM).

  • A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC50 = 14.2 µM).

  • Tenoxicam

    Cayman Chemical

    An NSAID that acts as a COX-2 inhibitor (IC50s = 20 and 322 nM for COX-1 and COX-2, respectively).

  • Bisindolylmaleimide V

    Cayman Chemical

    A weak inhibitor of PKC demonstrating an IC50 value >100 µM; blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.

  • BSI-201

    Cayman Chemical

    An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

  • Epothilone A

    Cayman Chemical

    An antimicrotubule agent that binds to β-tubulin with a similar order of magnitude as the binding of paclitaxel to β-tubulin (IC50s = 2.3 and 3.6 µM, respectively); cytotoxic to human T-24 bladder carcinoma cells (IC50 = 0.05 µM in vitro).

  • Meclofenamate (sodium salt)

    Cayman Chemical

    A time-dependent, non-specific COX inhibitor with IC50 values of 1.5 and 9.7 µM for human recombinant COX-1 and COX-2, respectively.

  • 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;…

  • 5a-Androst-16-en-3-one

    Cayman Chemical

    A mammalian pheromone used to prime sexual behavior of sows in estrus for mating or artificial insemination; also used to study receptor-mediated odorant detection and the genetic basis for anosmias.

  • Cyclic di-GMP

    Cayman Chemical

    An important second messenger in bacteria involved in biofilm formation, motility, virulence, and cell cycling; also has functions in eukaryotic cells.

  • 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…

  • 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.

  • 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…

  • 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…

  • CITCO

    Cayman Chemical

    An agonist of human CAR (EC50 = 49 nM); induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes.

  • Isoniazid

    Cayman Chemical

    An antibiotic that acts as a prodrug that is converted to isonicotinic acyl-NADH complex, which inhibits mycolic acid biosynthesis; effective against several species of Mycobacterium, including M. tuberculosis.

  • An alkaline aluminum−sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury; inhibits thrombin activity (IC50 = 4.5 µM) and prevents FGF-2 binding to endothelial cells, inhibiting tumor growth in mouse…

  • Quercetin

    Cayman Chemical

    A flavonoid compound found in the bark and rinds of many plants and fruits.

  • Tigecycline

    Cayman Chemical

    A glycylcycline antibiotic with a broad spectrum of activity against many Gram-positive, Gram-negative, and anaerobic organisms, including many multidrug-resistant strains.

  • Leupeptin (hemisulfate)

    Cayman Chemical

    A reversible inhibitor of cysteine, serine, and threonine proteases; inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.

  • Clobenpropit (hydrobromide)

    Cayman Chemical

    A selective histamine H3 receptor antagonist that crosses the blood-brain barrier; inhibits histamine binding in rat brain with an ED50 value of 10.5 mg/kg.

  • Oleic Acid

    Cayman Chemical

    Oleic acid is a monounsaturated fatty acid and is one of the major components of membrane phospholipids. Oleic acid contributes about 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets. Oleic acid inhibits collagen-stimulated platelet…

  • An angiotensin metabolite that functions as a type 1 angiotensin II receptor agonist whereupon it can control hydroelectrolyte balance and demonstrates vasodilatory and anti-inflammatory actions in opposition to various adverse effects of angiotensin II.

  • Tianeptine (sodium salt)

    Cayman Chemical

    An atypical antidepressant with diverse actions, most notably on the glutamatergic system; attenuates glutamate release and modulates the function of AMPAR; acts as an agonist of the µ-opioid receptor (EC50s = 194 and 641 nM for human and mouse receptors, respectively).

  • Sitagliptin (phosphate)

    Cayman Chemical

    A potent inhibitor of DPP-4 (IC50 = 18 nM); orally active, rapidly absorbed, and inhibits DPP-4 in plasma; lowers fasting plasma glucose, glycosylated hemoglobin, and two-hour postprandial glucose levels in patients with type 2 diabetes.

  • Micafungin (sodium salt)

    Cayman Chemical

    An echinocandin antifungal that inhibits 1,3-β-D-glucan synthesis; has fungicidal activity against virtually all species of Candida, including those resistant to fluconazole, and is fungistatic against Aspergillus spp.

  • Grifolic Acid

    Cayman Chemical

    A selective partial agonist of GPR120 that induces ERK activation and intracellular calcium responses in mouse enteroendocrine STC-1 cells that express GPR120 endogenously.

  • BMX-IN-1

    Cayman Chemical

    An irreversible inhibitor of BMX (IC50 = 8 nM) and BTK (IC50 = 10.4 nM); inhibits the proliferation of Tel-BMX-transformed Ba/F3 prostate cancer cells (GI50 = 25 nM), as well as RV-1, DU-145, PC-3, and VCAP prostate cancer cell lines (GI50s = 2.54, 4.38,…

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