Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    A selective SIP1 agonist (EC50 = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC50 = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

  • A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, the…

  • Cayman Chemical

    A naturally occurring macrolide polyene used to treat fungal infections, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium (minimal inhibitory concentrations ~ 4-64 μM); also used in the food industry as a "natural" preservative.

  • Cayman Chemical

    A Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro (GI50s ~ 9nM); 50 mg/kg inhibits tumor growth in a human colon cancer xenograft model by ~50% compared to vehicle controls.

  • Cefaclor is a second generation β-lactam cephalosporin antibiotic. Cefaclor exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding proteins to prevent peptidoglycan synthesis and bacterial cell wall formation. Cefaclor also displays…

  • Cayman Chemical

    An analog of AEA that potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons; selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis; inhibits the transport of AEA with an IC50 value of 1 µM in rat…

  • Cayman Chemical

    An irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.

  • Cayman Chemical

    A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

  • An inhibitor of S1P lyase; treatment of mice (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs, resulting in reversible lymphopenia.

  • Cayman Chemical

    A thiophene carboximide derivative proposed to inhibit IKK2; likely to be useful in the treatment of inflammatory diseases and cancer.

  • Cayman Chemical

    A cell-permeable analog of FPP that potently inhibits FTase (IC50 = 50-75 nM), preventing farnesylation of Ras; does not inhibit geranylgeranyl transferase at similar concentrations (IC50 > 100 µM); blocks Ras-mediated transformation of NIH 3T3 cells.

  • A fluorogenic substrate for chitinases and chitotriosidases.

  • 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.

  • Cayman Chemical

    Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

  • Cayman Chemical

    A potent and selective inhibitor of DGAT-1 (IC50 = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

  • LKT Labs

    F0F1-ATPase and adenine nucleotide translocator inhibitor and GABA receptor antagonist. It prevents mitochondrial respiration and decreases sperm count and motility. Grade: ≥70%

  • Cayman Chemical

    An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

  • Largely acts a cell signaling intermediate; serving as substrate to produce IP5s, which can be further phosphorylated to produce Ins(1,2,3,4,5,6-)P6; also phosphorylated to produce phytic acid, which serves diverse roles in eukaryotic tissues; a poor activator of the Ins(1,4,5)-P3 receptor in vitro.

  • LKT Labs

    ß-Carotene is a red-orange terpene pigment originally found in various plants and fruits; it is a prodrug for vitamin A. ß-Carotene exhibits antioxidative, cytoprotective, anticancer, anti-inflammatory, anti-hyperlipidemic, and anti-obesity activities. ß-Carotene is used in research models to…

  • Cayman Chemical

    A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

  • Cayman Chemical

    An analog of adenosine monophosphate that has antiviral activity; converted by cellular enzymes to tenofovir diphosphate, an obligate chain terminator that inhibits the activity of HIV reverse transcriptase and HBV polymerase.

  • Bis(salicyl) fumarate is an aspirin analog that is used to induce hemoglobin chain crosslinks at lysine residues. This compound is used to study hemoglobin function in research models and may be used to develop treatments for sickle-cell anemia. This compound may exhibit anti-inflammatory,…

  • β-cembrenediol is a diterpene product found in tobacco plants and cigarette smoke. β-cembrenediol displays weak anticancer and antimicrobial activity, exhibiting some cytotoxicity in cellular models. Grade: ≥98%

  • Cayman Chemical

    A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

  • Cayman Chemical

    An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 µM; dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle arrest in colon cancer cells.

  • Cayman Chemical

    A selective inhibitor of NLRP3, blocking the release of IL-1β in macrophages primed with LPS and activated with ATP or nigericin (IC50 = 7.5 nM); active in vivo, blocking the production of IL-1β and enhancing survival in mouse models of multiple sclerosis and…

  • Benzydamine is a non-steroidal anti-inflammatory drug (NSAID) that also exhibits analgesic, anesthetic, and antibacterial activities. Benzydamine is clinically used to treat mucositis and sore throat. Unlike most NSAIDs, benzydamine inhibits prostaglandin synthetase, not cyclooxygenase (COX).

  • Cayman Chemical

    CAS Number: 940929-33-9 Molecular Formula: C31H33ClN2O3 • HCl Formula Weight: 553.5

  • Cayman Chemical

    C-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…

  • A synthetic intermediate used in glycosylation reactions.

  • Cayman Chemical

    A selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).

  • Cayman Chemical

    An internal standard for the quantification of PGA2 by GC- or LC-MS.

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