Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • NQDI-1

    Cayman Chemical

    A selective inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

  • Docosanoic acid

    Cayman Chemical

    A long-chain fatty acid that exists naturally as a triglyceride in canola, peanut, and marine animal oils as well as animal milk fats and peanut skins.

  • A phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.

  • GSK484 (hydrochloride)

    Cayman Chemical

    A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils.

  • Arachidoyl Ethanolamide

    Cayman Chemical

    A saturated fatty acyl ethanolamide devoid of classical (CB1/CB2) activity; does not bind to the murine CB1 receptor and does not compete with AEA as a substrate for FAAH; a non-CB receptor-mediated pharmacology is still being elucidated.

  • Caffeine, Anhydrous

    MP Biomedicals

    Caffeine is a well-known drug commonly used as a mild stimulant, found in dietary sources such as coffee, tea, and cocoa. A central nervous system stimulant believed to act through adenosine receptors and monoamine neurotransmitters. It is an adenosine receptor antagonist and adenosine…

  • FTY720 phenoxy-biotin

    Cayman Chemical

    A biotin-tagged analog of FTY720; methanol side chain of FTY720 that is targeted for phosphorylation by sphingosine kinases is retained, suggesting that it would likewise be phosphorylated in vivo.

  • 2-D08

    Cayman Chemical

    An inhibitor of sumoylation.

  • 1-Hexadecyl lysophosphatidic acid is an ether analog of LPA containing a hexadecyl group at the sn-1 position. LPA binds to five different GPCRs to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility.

  • Reveromycin A

    Cayman Chemical

    A spiroketal antibiotic that inhibits EGF mitogenic activity, displays antiproliferative activity against human tumor cells, and demonstrates antifungal activity; inhibits bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 µM.

  • Detomidine (hydrochloride)

    Cayman Chemical

    A selective α2-adrenoceptor agonist (Ki = 1.62 nM) that binds to α1-adrenoceptors with much weaker potency (Ki = 415 nM); primarily used as a sedative for horses in large animal veterinary medicine.

  • XE 991 (hydrochloride)

    Cayman Chemical

    A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC50 = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC50 = 0.6 µM); shows good in vivo potency and duration of action.

  • Clodronate is a first-generation non-nitrogen-containing bisphosphonate that is used clinically for its anti-resorptive activity. Clodronate generates formation of a non-hydrolysable ß-? ATP analog that inhibits mitochondrial ADP/ATP translocase and prevents mitochondrial oxygen consumption…

  • A potent, selective inhibitor of SPHK 1 with anti-proliferative activity; exhibits non-ATP-competitive inhibition of human recombinant GST-SPHK 1 with an IC50 value of 0.5 µM, with no inhibition against ERK2, PI3K or PKCα at concentrations up to 60 µM; inhibits proliferation of…

  • Lipoxin A4

    Cayman Chemical

    A trihydroxy fatty acid containing a conjugated tetraene produced by the metabolism of (±)15-HETE or 15-HpETE with human leukocytes; promotes leukocyte activation, chemotaxis effects, natural killer cell inhibition, and monocyte migration and adhesion.

  • ML-228

    Cayman Chemical

    An activator of the HIF signaling pathway, as demonstrated by HRE reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM); activity is blocked by excess iron,…

  • 8(S)-HEPE

    Cayman Chemical

    8(S)-HEPE is a monohydroxy fatty acid produced by lipoxygenase oxidation of EPA. It acts to promote hatching of barnacle eggs at 10 nM, although it is not clearly identified as the natural egg hatching factor.

  • Sodium Valproate

    MP Biomedicals

    Valproic Acid, Sodium Salt is a branched chain fatty acid which is reported to enhance central GABAergic neurotransmission and inhibit Na+ channels. Sodium Valproate is reported to cause inositol depletion, activate the ERK pathway, inhibit GSK-3α and GSK-3β. Valproic Acid has been…

  • Sodium dodecyl sulfate (SDS) 10% (w/v) stock solution contains 10% sodium dodecyl sulfate. It is ready to use as supplied.

  • (R)-benzyl Mandelate

    Cayman Chemical

    (R)-benzyl Mandelate is a synthetic intermediate useful for pharmaceutical synthesis.

  • Ophiobolin C

    Cayman Chemical

    A phytoxin that antagonizes chemokine receptor CCR5 binding (IC50 = 40 µM) to the envelop protein gp120 and to CD4, which is known to mediate HIV-1 viral entry into cells; cytotoxic to CLL cells (LC50 = 8 nM).

  • 14,15-Leukotriene C4

    Cayman Chemical

    A unique LT with weak contractile activity on both guinea pig ileum and pulmonary parenchyma compared to 5-LO-derived LTs; increases vascular permeability of human endothelial cell monolayers with similar potency to that of 5-LO-derived LTs.

  • PPQ-102

    Cayman Chemical

    A cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels (IC50 = 90 nM); reduces the size and number of renal cysts in a neonatal kidney organ culture model of polycystic kidney disease; increases VEGF-A production in cultured airway epithelial…

  • 17-Octadecynoic Acid

    Cayman Chemical

    A suicide inhibitor of LTB4 20-hydroxylase and renal CYP450 ω-hydroxylase.

  • 5-OxoETE-d7

    Cayman Chemical

    An internal standard for the quantification of 5-oxoETE by GC- or LC-MS.

  • Carbetapentane (citrate)

    Cayman Chemical

    An agonist of the sigma-1 receptor (Ki = 10.4 nM); also binds the serotonin 5-HT3 and muscarinic acetylcholine receptors (Kis = 7.9 and 76 nM, respectively).

  • Aflatoxin B1

    Cayman Chemical

    Naturally occuring mycotoxin and food contaminant that induces the transversion of G to T at codon 249 of the p53 tumor suppressor gene and is a likely pathogen that causes hepatocellular carcinoma.

  • Amrinone

    LKT Labs

    Amrinone is a pyridine phosphodiesterase 3 (PDE 3) inhibitor that is clinically used to treat congestive heart failure (CHF). Amrinone may be administered during cardiopulmonary bypass surgery. Amrinone exhibits positive inotropic activity, inducing vasodilation and increasing cardiac contractility…

  • Pimonidazole

    Cayman Chemical

    A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.

  • Cycloguanil (hydrochloride)

    Cayman Chemical

    An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

  • KN-92 (hydrochloride)

    Cayman Chemical

    An inactive derivative of KN-93, the selective inhibitor of CaMKII; ineffective at inhibiting CaMKII or arresting cell growth of NIH 3T3 fibroblasts at concentrations up to 25 μM.

  • Angiotensin peptides exhibit pressor (vasoconstrictive) activity through binding of the angiotensin II type 1 (AT1) receptor, increasing blood pressure and volume. Angiotensin I (AT I) is a cleavage product of angiotensin and serves no primary biological purpose other than to function as a…

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