Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • Zatebradine (hydrochloride)

    Cayman Chemical

    Blocks If currents through HCN channels in sinoatrial node cells (IC50s = 1.83, 2.21, 1.9, and 1.88 µM, respectively for HCN1-4 in vitro); reduces heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induces increasing arrhythmia at…

  • Cafestol

    Cayman Chemical

    A natural diterpene which elevates serum cholesterol and triglycerides in humans, an effect which does not seem to occur in monkeys, hamsters, rats or gerbils; increase total cholesterol and triglycerides in ApoE3Leiden mice, an effect which is associated with selective activation of FXR and PXR.

  • A-61603

    Cayman Chemical

    A selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D; increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro with 330-fold more potency compared to activation by phenylephrine.

  • Hesperetin

    Cayman Chemical

    The flavones and flavonoids are a widespread group of natural products with a variety of reported beneficial health effects. Flavonoids have been implicated as possible active agents in the dietary benefits of citrus fruits. Hesperetin is a citrus flavonoid that has been reported to lower plasma…

  • ESI-09

    Cayman Chemical

    A inhibitor of Epac1 and Epac2 (IC50s = 3.2 and 1.4 µM, respectively); blocks Akt phosphorylation and insulin secretion in pancreatic β cells and inhibits the migration of AsPC-1 and PANC-1 pancreatic cancer cells in vitro.

  • Sulprostone

    Cayman Chemical

    Sulprostone is a metabolism resistant synthetic analog of PGE2. It is a selective agonist for EP3 receptors with a Ki value of 0.35 nM at the human recombinant EP3-III receptor and an IC50 of 0.01 µM for the inhibition of PGE2 binding. Sulprostone is a potent stimulator of uterine…

  • (±)11(12)-EET methyl ester

    Cayman Chemical

    A more stable form of (±)11(12)-EET used for long-term storage.

  • LRRK2-IN-1

    Cayman Chemical

    A potent, selective inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC50s = 13 and 6 nM, respectively); stimulates macroautophagy in H4 neuroglioma cells.

  • Harzianopyridone

    Cayman Chemical

    A natural inhibitor of mitochondrial complex II with antibiotic activities.

  • D-erythro-Sphinganine

    Cayman Chemical

    D-erythro-Sphinganine is a precursor of ceramide and sphingosine as well as a substrate of sphingosine kinases, which generate sphinganine-1-phosphate. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins, as well as in some cancers. Sphinganine can…

  • Perlapine

    Cayman Chemical

    An atypical neuroleptic that blocks dopamine and serotonin (5-HT) receptors (Kis = 60, 30, and 30 nM for D2, D4, and 5-HT2A, respectively); an agonist for hM3Dq, a DREADD, with >10,000-fold selectivity for hM3Dq over hM3.

  • Spinosyn D

    Cayman Chemical

    An agonist of insect nicotinic acetylcholinesterase receptors that demonstrates insecticidal activity against H. virescens larvae (tobacco budworm) with an LD50 value of 0.8 ppm.

  • Cryptotanshinone

    Cayman Chemical

    A natural quinoid diterpene that, at 10-20 µM, stimulates AMPK in C2C12 myotubes and activates p38 MAPK in DU145 cells; inhibits SHP2 in vitro (IC50 = 22.5 µM) and, at 4-8 µM, blocks phosphorylation of STAT3 in MC-3 cells; has a variety of anti-cancer actions.

  • S32826

    Cayman Chemical

    A potent and selective inhibitor of autotaxin, inhibiting recombinant autotaxin β with an IC50 value of 8.8 nM; inhibits LPA release from adipocytes (IC50 = 90 nM) and reduces plasma autotaxin activity by 57% when used at 5 μM.

  • BIX 02565

    Cayman Chemical

    A potent RSK2 inhibitor (IC50 = 1.1 nM) that also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic ?1A, ?1B, ?1D, ?2A, β2, and imidazoline I2…

  • Heneicosapentaenoic Acid-d6

    Cayman Chemical

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

  • 8-iso-17-phenyl trinor Prostaglandin F2ß

    Cayman Chemical

    8-iso-17-phenyl PGF2β is an isomer of bimatoprost (free acid) that is epimerized at the 8 and 9 positions. There are no published reports on the biological activity of 8-iso-17-phenyl PGF2β.

  • 5-trans Fluprostenol isopropyl ester

    Cayman Chemical

    Travoprost is the Alcon trade name for fluprostenol isopropyl ester, an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. Fluprostenol isopropyl ester is a prodrug which is converted by esterase enzymatic activity in the cornea to yield the corresponding…

  • Fexinidazole

    Cayman Chemical

    An antiparasitic drug that, in different preparations, is effective against trypanosomes; orally available and rapidly metabolized to two active metabolites.

  • EBPC

    Cayman Chemical

    A potent, selective inhibitor of aldose reductase (IC50 = 47 nM in vitro) used to improve the cytotoxic effects certain anticancer agents; inhibits PGF2α and PGE2 production in human endometrial cells (EC50 = 10 μM).

  • P7C3

    Cayman Chemical

    An orally bioavailable and brain penetrant aminopropyl carbazole that exhibits proneurogenic and neuroprotective activity by preventing apoptosis of newly postmitotic neurons in the subgranular zone of the hippocampal dentate gyrus; promotes survival of neurons in various rodent models of…

  • Pirfenidone

    Cayman Chemical

    An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

  • SIRT1/2 Inhibitor IV

    Cayman Chemical

    A cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM); less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a…

  • Palonosetron (hydrochloride)

    Cayman Chemical

    A potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex); orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs; remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life.

  • Foretinib

    Cayman Chemical

    Foretinib is a broad-spectrum tyrosine kinase (TK) inhibitor that targets members of the HGF and VEGF receptor TK families, as well as KIT, Flt-3, PDGFRβ, and Tie-2, at nanomolar concentrations. It blocks HGF-induced Met phosphorylation and VEGF-induced ERK phosphorylation, preventing…

  • CAY10594

    Cayman Chemical

    A potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM); also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells); strongly inhibits the invasive migration of breast cancer cells in…

  • Nervonic Acid

    Cayman Chemical

    A very long chain fatty acid (24:1n-9) enriched in nervous tissue and particularly abundant in sphingolipids, such as sphingomyelin; poorly produced in demyelinating disorders, including multiple sclerosis and adrenoleukodystrophy; binds and inhibits DNA polymerase β (Ki = 4.0 uM) and HIV-1…

  • SGI-1027

    Cayman Chemical

    An inhibitor of the DNA methyltransferases DNMT1, DNMT3A, and DNMT3B (IC50s = 12.5, 8, and 7.5 μM, respectively, with Poly(dI-dC) as the substrate); reactivates silenced tumor suppressor genes by reducing CpG island hypermethylation.

  • 18-carboxy dinor Leukotriene B4

    Cayman Chemical

    A β-oxidation metabolite of LTB4.

  • DG-172 (hydrochloride)

    Cayman Chemical

    An orally available inverse agonist of PPARβ/δ (IC50 = 27 nM), down-regulating transcription of ANGPTL4 in mouse myoblasts (IC50 = 9.5 nM).

  • Calcein AM

    Cayman Chemical

    A cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.

  • S18886

    Cayman Chemical

    An orally active, long-acting antagonist of the TP receptor (IC50 = 16.4 nM); inhibits TP receptor-mediated vascular contractions, platelet aggregation, and adhesion and infiltration of monocytes/macrophages in various pre-clinical and clinical models of thrombosis or atherosclerosis.

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