Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • W-5 (hydrochloride)

    Cayman Chemical

    A less active, chlorine-deficient analog of W-7, the potent calmodulin antagonist (Ki = 11 μM); suitable for use as a control compound for understanding the specificity of other calmodulin antagonists.

  • A phospholipid in which the two acyl substituents at positions sn-1 and sn-2 are specified as palmitoyl (16:0) and lauroyl (12:0), respectively.

  • Citrinin

    Cayman Chemical

    A mycotoxin found as food contaminants that causes mycotoxic nephropathy in livestock and Balkan nephropathy and yellow rice fever in humans; induces apoptosis, blocks tubulin polymerization, and disrupts mitotic spindle assembly.

  • PGF2α isopropyl ester is an ester prodrug of PGF2α with enhanced lipid solubility. Due to better membrane penetration, PGF2α isopropyl ester is more suitable than PGF2α or PGF2α tromethamine salt for topical application in studies on intraocular pressure. The ester…

  • RAD140

    Cayman Chemical

    AD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM. At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats. At…

  • TTNPB

    Cayman Chemical

    An analog of retinoic acid that potently and selectively activates retinoic acid receptors (EC50s = 21, 4, and 2.4 nM for RARα, RARβ, and RARγ, respectively); used to study RAR action in epidermal cell proliferation, embryogenesis, and stem cell differentiation.

  • 2-O-methyl PAF C-18

    Cayman Chemical

    A synthetic PAF analog which contains an ether-linked methyl group at the sn-2 position; decreases plasma membrane fluidity, inhibits tumor cell invasiveness, and causes the release of large quantities of NO by a pathway involving activation of NOS.

  • RHC-80267

    Cayman Chemical

    A selective inhibitor of diacylglycerol lipase (IC50 = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C; elevates the concentration of diacylglycerol, which leads to activation of PKC.

  • A C34:6 VLCPUFA whose specific biological actions are largely unknown.

  • HA-14-1

    Cayman Chemical

    A small molecule inhibitor of Bcl-2 proteins (IC50 = ~ 9 µM) that induces apoptosis of human acute myeloid leukemia (HL-60) cells (50 µM induces 90% loss of viability).

  • Purvalanol B

    Cayman Chemical

    A CDK inhibitor that most potently inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdc2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively); inhibits the growth of parasites, including Plasmodium, at micromolar doses.

  • Sulfasalazine

    Cayman Chemical

    A prodrug of 5-aminosalicylic acid that is used to treat inflammatory bowel disease and rheumatoid arthritis because of its ability to induce T lymphocyte apoptosis, modulate inflammatory mediators from both COX/5-LO pathways and NF-κB signaling pathways, attenuate transcription of…

  • 6-fluoro-DL-Tryptophan

    Cayman Chemical

    A serotonin synthesis inhibitor that is used for tracing pools of neuronal serotonin, as a competitive inhibitor of tryptophan binding to albumin, and as a substrate for the serotonin neural transporter.

  • NVP-BHG712

    Cayman Chemical

    A selective, orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 =25 nM); inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.

  • Dibenzylfluorescein

    Cayman Chemical

    A fluorogenic probe that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19); used to detect changes in CYP catalytic activity caused by drugs or disease.

  • EPZ6438

    Cayman Chemical

    An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their…

  • Zerumbone

    Cayman Chemical

    A natural monocyclic sesquiterpene that potently inhibits the activation of Epstein-Barr virus by phorbol esters (IC50 = 140 nM); inhibits SHH signaling and induces apoptosis in cancer cell lines.

  • AS-703026

    Cayman Chemical

    Selectively inhibits MEK1/2; potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively); 30 mg/kg reduced tumor growth significantly in mice bearing H929 MM xenografts.

  • 7(Z)-Pentacosene

    Cayman Chemical

    An unsaturated cuticular hydrocarbon that acts as a contact sex pheromone in Drosophila; may stimulate copulation either by itself at high concentrations or when combined with other alkenes; increases in Drosophila females immediately after copulation.

  • Cyproterone Acetate

    Cayman Chemical

    An antagonist/partial agonist of the androgen receptor (IC50 = 26 nM in humans) that has been shown to have clinical use in androgen-dependent conditions such as prostate cancer, hirsutism, and alopecia; suppresses accessory sexual glands and fertility in adult male rats (10…

  • Rosuvastatin (calcium salt)

    Cayman Chemical

    An HMG-CoA reductase inhibitor (IC50 = 5 nM); reduces low-density lipoprotein and C-reactive protein and increases high-density lipoprotein in clinical trials.

  • 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…

  • RGFP966

    Cayman Chemical

    A selective inhibitor of HDAC3 (IC50 = 0.08 µM) that does not affect other HDACs at concentrations up to 15 µM; enhances long-term object memory acquisition/consolidation in mice; induces apoptosis of cutaneous T cell lymphoma cells by disrupting their DNA replication activity.

  • 5-trans Prostaglandin F2ß

    Cayman Chemical

    A 9β-hydroxy isomer of 5-trans PGF2α.

  • An analog of PGF2α in which the C-1 carboxyl group has been modified to an N-diethyl that is inert to coneal amidase activity.

  • NKY80

    Cayman Chemical

    A cell-permeable, selective adenylyl cyclase type V inhibitor (IC50 = 8.3 μM in the presence of Gsα GTPγS-forskolin); tissue selective for the adenylyl cyclase catalytic activity in heart and lung tissues.

  • Glipizide

    Cayman Chemical

    A short-acting, second-generation, blood-glucose-lowering agent belonging to the sulfonylurea class that increases the release of endogenous insulin; commonly used to lower blood sugar levels in type 2 diabetes (non-insulin-dependent diabetes).

  • An isomer of 17-phenyl trinor PGF2α ethyl amide wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E); an impurity in commercial preparations of the bulk drug product.

  • Hexa-N-acetylchitohexaose

    Cayman Chemical

    A hexamer of N-acetylglucosamine that functions as an elicitor in plants, inducing the expression of chitinases; a substrate of lysozyme; binds LysM domains on certain proteins, including an endopeptidase of T. thermophilus.

  • 3-Pyrimidin-2-yl-2-pyrimidin-2-ylmethyl-propionic acid is a synthetic intermediate useful for pharmaceutical synthesis.

  • (±)13-HDHA

    Cayman Chemical

    (±)13-HDHA is an autoxidation product of DHA in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. Fresh water hydra was shown to metabolize DHA to 13(R)-HDHA, presumably via 11(R)-LO. (±)13-HDHA is a potential marker of oxidative stress…

  • Prasugrel

    Cayman Chemical

    A thienopyridine prodrug that is converted by esterases to a receptor antagonist for purinergic P2Y12 receptors, preventing platelet aggregation.

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