Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • A high affinity ligand of CB2 (Ki = 8.5 nM) with little affinity for CB1 (Ki >10000 nM); demonstrates antinociceptive efficacy in the mouse formalin test at 1 mg/kg, an action which is blocked by a CB2-selective antagonist, AM630.

  • Q-VD-OPH

    Cayman Chemical

    A broad spectrum caspase inhibitor, blocking caspases-3, -7, -8, -9, -10, and -12 and inhibiting apoptosis when used at 10 µM; more effectively inhibits apoptosis and is much less cytotoxic than Z-VAD-FMK; can be used in vivo.

  • A derivative of PGF2β with increased water solubility.

  • (S)-(+)-Methoprene

    Cayman Chemical

    A widely-used insect growth regulator; acts as an activator of the juvenile hormone receptor, known as Methoprene-tolerant, or Met (Kd = 12.3 nM).

  • An optically active isomer of TBP-OH, a compound produced from the metabolism of the organophosphorus solvent, TBP.

  • A nucleotide that upon phosphorylation to GTP becomes incorporated into RNA; used to study modulation of glutamatergic neurotransmission.

  • L-Arginine

    LKT Labs

    L-Arginine is an endogenous amino acid also found in meat, dairy, grains, and legumes. L-Arginine exhibits vasodilatory and antihypertensive activities, as it is a precursor to the formation of NO. L-Arginine decreases systolic and diastolic blood pressure, improving cardiovascular and endothelial…

  • CPHPC

    Cayman Chemical

    A divalent crosslinker of SAP that causes rapid depletion of circulating SAP via hepatic clearance.

  • Suc-Leu-Leu-Val-Tyr-AMC

    Cayman Chemical

    A fluorescent substrate for the 20S proteasome, other chymotrypsin-like proteases, and calpains (excitation max: 360 nm; emission max: 460 nm).

  • CVT-10216

    Cayman Chemical

    A selective, reversible inhibitor of ALDH2 (IC50 = 29 nM); reduces excessive alcohol drinking in alcohol-preferring rats, prevents self-administration of alcohol in Long-Evans rats, and produces anxiolytic effects.

  • Salicin

    Cayman Chemical

    An alcoholic β-glucoside derived from willow bark that produces anti-inflammatory (including analgesic and antipyretic) effects similar to that of aspirin by non-selectively inhibiting COX-1 and COX-2 (IC50s > 100 µM).

  • Oligomycin E

    Cayman Chemical

    A minor metabolite of the oligomycin complex that is active against Gram-positive bacteria and demonstrates strong antitumor activity against HeLa cells (IC50 = 14 ng/ml).

  • AEBSF (hydrochloride)

    Cayman Chemical

    A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

  • JNJ-10397049

    Cayman Chemical

    A potent, selective, and bioavailable antagonist of the OX2R (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R); decreases the latency to persistent sleep and increases persistent sleep time when applied subcutaneously to rats.

  • 17-phenyl trinor 8-iso PGE2 is the C-8 epimer of 17-phenyl trinor PGE2, a synthetic analog of PGE2. 17-phenyl trinor PGE2 is an EP1 and EP3 receptor agonist that causes contraction of the guinea pig ileum at a concentration of 11 µM. There are no published studies of the pharmacological…

  • A metabolite of lipoxygenase-mediated oxidation of DPA; activates Nrf2-dependent antioxidant gene expression, acts as a PPARγ agonist (EC50 = ~200 nM), and inhibits pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 µM).

  • AP26113

    Cayman Chemical

    An orally bioavailable inhibitor of ALK (IC50 < 100 nM in Ba/F3 cells); a pan-ALK inhibitor that also inhibits several ALK mutants that confer resistance to other ALK inhibitors.

  • A substrate of S1P lyase, leading to the production of the fluorescent product umbelliferone; intended to be used to monitor or measure S1P lyase activity.

  • Butaprost (free acid)

    Cayman Chemical

    A potent, selective EP2 receptor agonist (Ki = 73 nM).

  • w-3 Arachidonic Acid

    Cayman Chemical

    ω-3 Arachidonic acid is a rare PUFA found in trace amounts in dietary sources. ω-3 Fatty acids are now known to be essential for infant growth and development and protect against heart disease, thrombosis, hypertension, and inflammatory and autoimmune disorders. In human platelet…

  • Panobinostat

    Cayman Chemical

    A potent inhibitor of all HDACs, with Ki values ranging from 0.6 to 31 nM for HDAC1-11; leads to acetylation of a range of cellular proteins, resulting in cell cycle arrest and apoptosis in cancer cells; has potential applications in spinal muscular atrophy and HIV therapy.

  • Kobe 2602

    Cayman Chemical

    A selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM); inhibits both anchorage-dependent and -independent growth and induces apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = 1.4-2 µM).

  • ML-297

    Cayman Chemical

    A selective GIRK1/2 activator (EC50s = 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively; 60 mg/kg can delay seizure onset and prevent convulsions in two different mouse models of epilepsy.

  • Ac-DEVD-AFC

    Cayman Chemical

    A fluorogenic substrate for activated caspase-3 (Km = 9.7 µM), as well as related caspases; caspase activity can be quantified by fluorescent detection of free AFC, which is excited at 400 nm and emits at 505 nm.

  • Bepridil (hydrochloride)

    Cayman Chemical

    A dihydropyridine that has anti-anginal and anti-arrhythmic actions by blocking calcium channels in heart and smooth muscle; recognized as a non-selective channel blocker.

  • FG-2216

    Cayman Chemical

    An orally active PHD2 inhibitor (IC50 = 3.9 µM); stabilizes HIF-α and reversibly stimulate erythropoietin secretion at 100 µM in vitro; increases hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.

  • Doxofylline

    Cayman Chemical

    A methylxanthine bronchodilator that inhibits phosphodiesterase activity and, thus, increases cAMP; demonstrates decreased affinity towards adenosine A1 and A2 receptors, does not interfere with calcium influx into cells, and does not antagonize the action of calcium-channel blockers.

  • Besifloxacin is a fourth generation fluoroquinolone antibiotic that displays broad-spectrum antibacterial activity against aerobic and anaerobic bacteria and is effective against a wide range of ocular pathogens that exhibit resistance to other fluoroquinolone antibiotics. Besifloxacin inhibits DNA…

  • GSK3787

    Cayman Chemical

    A selective, irreversible antagonist of PPARβ/δ (pIC50 = 6.6) that inhibits the expression of PPARβ/δ-regulated target genes, PDK4, CPT1a, and Angptl4.

  • Paprotrain

    Cayman Chemical

    A selective, cell-permeable, reversible inhibitor of MKLP-2 (IC50s = 0.83-1.35 μM); treatment with 10-50 μM results in binucleated cells, perturbing relocation of Aurora B kinase and survivin to the central spindle in anaphase cells without affecting microtubule polymerization.

  • Ampkinone

    Cayman Chemical

    A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

  • GSK4112

    Cayman Chemical

    A synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that mimics the action of heme; at 10 μM inhibits the expression of the circadian target gene bmal1 and reduces glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.

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