Biologically Active Small Molecules

Laboratory Chemicals - Life Science - Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Apramycin is an aminoglycoside antibiotic originally produced by Streptomyces. Apramycin is clinically used in veterinary medicine. This compound binds 16S rRNA of the bacterial 30S ribosomal subunit, causing conformational changes in CA and GA base pairs and inhibiting RNA translocation.

  • Cayman Chemical

    An indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells.

  • LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

  • An antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM); inhibits ADP-induced platelet aggregation ex vivo; shown to be beneficial in the prevention of vascular ischemic events for patients without…

  • Cayman Chemical

    A chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21); potent in cells, with an IC50 value of 250 nM.

  • Cayman Chemical

    An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

  • Cayman Chemical

    A potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

  • Tris-HCl Stock Solution (1 M, pH 7.0) contains filtered Tris-HCl (1 M, pH7.0). It is ready to use as supplied.

  • Cayman Chemical

    A class III antiarrhythmic agent; inhibits KCNH2 with an IC50 value of 1 µM; also inhibits CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.

  • Cayman Chemical

    Differs from the major microcystin variant LR with the substitution of alanine in place of the arginine; inhibits both PP1C and PP2A with an IC50 value of 0.3 nM.

  • Cayman Chemical

    An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

  • Cayman Chemical

    A major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.

  • A long-acting ascorbic acid derivative that stimulates collagen expression and formation and is used in human cell culture; included in media to enhance the survival of human embryonic stem cells or drive osteogenic differentiation in human adipose stem cells and in human mesenchymal stromal/stem cells.

  • Berberine is an isoquinoline alkaloid found in a variety of plants, including barberry, goldenseal, Oregon grape, California poppy, and the Amur cork tree. Berberine fluoresces under ultraviolet light and is often used to stain heparin in mast cells. Berberine displays many beneficial effects,…

  • Cayman Chemical

    A major metabolite of PGD2 found in human and mouse urine at levels of approximately 1.5 and 8.1 ng/mg creatinine, respectively.

  • Cayman Chemical

    A monoamine neurotransmitter produced in serotonergic neurons in the CNS and in enterochromaffin cells in the gastrointestinal tract that is important in the regulation of mood, sleep, vomiting, sexuality, and appetite.

  • An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

  • Cayman Chemical

    A derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

  • Cayman Chemical

    An antifungal antibiotic that selectively inhibits succinate dehydrogenase (complex II; IC50s = 12 and 3.7 nM in nematode and mammalian mitochondria, respectively, versus IC50s > 100 μM for inhibition of complex I and complex III enzymes); has cardioprotective effects against simulated…

  • 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…

  • 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.

  • Cayman Chemical

    An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC50 = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

  • Cayman Chemical

    This solution can be used (without further dilution) as a blocking agent for immunocytochemistry or immunohistochemistry when using a secondary antibody generated in goat.

  • Cayman Chemical

    A positive modulator of the small conductance calcium-activated potassium channels SK2 and SK3 (EC50s = 14 and 5.6 µM, respectively); inactive on both SK1 and IK; increases the apparent calcium-sensitivity of channel activation of SK3, changing the EC50 value of calcium…

  • Cayman Chemical

    A natural adenosine analog that prevents IRE1α-induced mRNA cleavage (IC50 = 80 nM) and inhibits constitutive activation of XBP1 in multiple myeloma cell lines; used to study IRE1α action in the endoplasmic reticulum stress response.

  • Cayman Chemical

    A selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC50 = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC50 = 52.8 nM) but not κ/δ or μ/κ heteromers.

  • Cayman Chemical

    A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC50s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

  • A phospholipid containing the saturated long-chain (18:0) stearic acid inserted at the sn-1 and sn-2 positions.

  • LKT Labs

    Bilobalide is a sesquiterpene lactone found in Ginkgo that exhibits neuroprotective, cognition enhancing, anxiolytic, antioxidative, anti-inflammatory, and analgesic activities. Bilobalide inhibits GABA-A receptors, decreases anxiety, and improves spatial learning and memory in vivo. In animal…

  • Cayman Chemical

    A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

  • Cayman Chemical

    PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC50 of PGE1 for the inhibition of ADP-induced human platelet…

  • Cayman Chemical

    An inactive analog of U-73122; can be used as a negative control.

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