Biologically Active Small Molecules

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UN2811 Cayman Chemical Biologically Active Small Molecules

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  • L-779,450

    Cayman Chemical

    An ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that inhibits cell proliferation both in B-Raf mutated and wild-type melanoma cell lines.

  • KT195

    Cayman Chemical

    A selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.

  • Citreoviridin

    Cayman Chemical

    A mycotoxin that inhibits the mitochondrial ATP synthetase system; inhibits soluble ATPase (KD = 4.1 µM), ADP-stimulated respiration in isolated rat liver mitochondria (KD = 0.15 µM), and ATP-driven reduction of NAD+ by succinate (KD = 2 µM).

  • Flibanserin

    Cayman Chemical

    A full agonist of the serotonin 5-HT1A receptor and antagonist of 5-HT2A (Kis = 1 and 49 nM, respectively); also binds to dopamine D4 receptors (Kis = 4-24 nM); reduces 5-HT in the prefrontal cortex and dorsal raphe of conscious rats while increasing extracellular noradrenaline and dopamine.

  • Antimycin A1

    Cayman Chemical

    An antibiotic that inhibits complex III of the mitochondrial ETC, preventing electron transport between cytochromes b and c, which results in the production of superoxide and eventual cell death; inhibits Bcl-2 and Bcl-xL proteins, inducing apoptosis.

  • PF-06447475

    Cayman Chemical

    An LRRK2 inhibitor (IC50 = 3 nM) that has been shown to attenuate α-synuclein-induced dopaminergic neurodegeneration and neuroinflammation in G2019S-LRRK2-expressing rats.

  • Colcemid

    Cayman Chemical

    A colchicine derivative that inhibits tubulin polymerization (IC50 = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

  • Epinastine (hydrochloride)

    Cayman Chemical

    A non-sedating ophthalmic antihistamine that antagonizes histamine H1 receptors (IC50 = 1.58 nM) and prevents the release of pro-inflammatory mediators from mast cells and eosinophils.

  • Nicardipine (hydrochloride)

    Cayman Chemical

    A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

  • Inauhzin

    Cayman Chemical

    A cell-permeable, selective SIRT1 inhibitor (IC50 = 0.7-2 µM) that reactivates p53 by inhibiting SIRT1 deacetylation activity; inhibits cell proliferation by inducing p53-dependent apoptosis in various human cancer cells (IC50s = 5.4, 51.9, 3.2, 33.9, and 85.4 µM…

  • CI-994

    Cayman Chemical

    An inhibitor of class I HDACs with IC50 values of 0.9, 0.9, 1.2, and >20 μM for recombinant human HDAC 1, 2, 3, and 8, respectively; displays a wide spectrum of antitumor activity, particularly in tumors normally refractory to conventional anticancer agents.

  • Cytochalasin E

    Cayman Chemical

    Inhibits actin polymerization; potently and selectively inhibits the growth of endothelial cells (IC50 1 protease activity.

  • Tacrine (hydrochloride)

    Cayman Chemical

    A derivative of aminoacridine that functions as an inhibitor of both AChE and butyrylcholinesterase; used clinically in the treatment of Alzheimer’s disease; inhibits the uptake of serotonin and noradrenaline in rat cerebral cortex and decreases depolarization-induced calcium influx through…

  • Vincristine (sulfate)

    Cayman Chemical

    An antimitotic vinca alkaloid which irreversibly blocks mitosis by binding to tubulin (Ki = 85 nM) and inhibiting tubulin polymerization; exported from cells via the ABC transporter P-glycoprotein but not by Mrp1.

  • Rivastigmine (tartrate)

    Cayman Chemical

    An irreversible inhibitor of AChE (IC50 = 4.15 µM) and BuChE (IC50 = 37 nM); used in modifying the course of neurodegenerative diseases.

  • Clonidine (hydrochloride)

    Cayman Chemical

    A centrally acting α2-adrenergic receptor agonist that decreases peripheral vascular resistance by centrally inhibiting sympathetic nerve activity; also acts as an agonist of the imidazoline (I1) receptor (Ki = 4-8 nM).

  • Paxilline

    Cayman Chemical

    An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

  • 1,25-dihydroxy Vitamin D2

    Cayman Chemical

    The active circulating metabolite of vitamin D2 formed by 25-hydroxylase in the liver and 25-hydroxyvitamin D-hydroxylase in the kidney.

  • (+)-Warfarin

    Cayman Chemical

    An anti-coagulant; differs from (−)-warfarin by being five times less potent as a vitamin K antagonist; has a longer terminal elimination half-life (35-58 hours) than (−)-warfarin (24-33 hours).

  • Benzbromarone

    Cayman Chemical

    An inhibitor of URAT1 (IC50 = 0.3 µM for hURAT1) that prevents renal urate resorption; also potently inhibits CYP2C9 (Ki = 20 nM) and has been used to study adverse drug-drug interactions.

  • 7-Nitroindazole

    Cayman Chemical

    A non-selective inhibitor of NOS isoforms in vitro (IC50s = 0.71, 0.78, and 5.8 µM for rat nNOS, bovine eNOS, and rat iNOS, respectively); shows good anti-nociceptive effects without affecting blood pressure via inhibition of eNOS in vivo.

  • Vitamin D3

    Cayman Chemical

    An intermediate form of vitamin D which is obtained from dietary sources, such as fish, or through the conversion of 7-dehydrocholesterol by ultraviolet light; metabolized to the active form 1,25-dihydroxyvitamin D3 by CYP450 isoforms in the liver.

  • Valinomycin

    Cayman Chemical

    A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

  • Voriconazole

    Cayman Chemical

    A triazole, antifungal agent that inhibits a broad range of pathogenic yeasts, including Candida (MIC = 0.03-8 µg/ml), and filamentous fungi such as Aspergillus, Scedosporium, and Fusarium by disrupting ergosterol synthesis.

  • P005091

    Cayman Chemical

    A trisubstituted thiophene that selectively inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively); accelerates the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 =11 μM).

  • Resiniferatoxin

    Cayman Chemical

    A natural analog of capsaicin that activates TrpV1 with a Ki value of 20 pM; potently and selectively activates of a sub-population of primary afferent neurons.

  • Tenuazonic Acid

    Cayman Chemical

    A major Alternaria mycotoxins commonly found as a food contaminant (LD50 = 548 μg/egg in the chicken embryo toxicity assay) and linked to esophageal cancer in human populations at risk of high exposure; Mice fed 100 mg/kg/day orally for 10 months developed precancerous lesions on the esophageal mucosa.

  • Oxytocin

    Cayman Chemical

    A nonapeptide hormone primarily synthesized in the hypothalamus with roles in uterine contraction and lactation, social memory and attachment, sexual and maternal behavior, aggression, learning, anxiety, feeding, and pain perception.

  • Carazolol

    Cayman Chemical

    A high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors (Kis = 0.114 and 0.4 nM for β2- and β3-adrenoceptors, respectively); acts as a receptor antagonist (beta blocker) or inverse agonist for β1 and β2 receptors but functions as an agonist at the…

  • 5-Fluorouracil

    Cayman Chemical

    A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

  • Diclofenac-d4

    Cayman Chemical

    Intended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.

  • Capsaicin

    Cayman Chemical

    The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

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