Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Ascomycin

    Cayman Chemical

    An ethyl analog of tacrolimus with potent immunosuppressant properties that prevents T-cell proliferation through initial binding to FKBP12, the principal mediator of FK506- and rapamycin-induced immunosuppression; inhibits the enzymatic PPIase and chaperone activities of PfFKBP35 (IC50 = 0.52…

  • 17-Allylaminogeldanamycin

    LKT Labs

    Geldanamycin derivative and HSP90 inhibitor. It induces apoptosis in cancer cells and inhibits replication of cytomegalovirus.

  • trans-trismethoxy Resveratrol

    Cayman Chemical

    An analog of resveratrol in which the three phenolic hydroxyl groups of resveratrol are converted to methyl ethers; exhibits enhanced inhibition of cell growth and pro-apoptotic activities compared to resveratrol.

  • Sodium 4-Phenylbutyrate

    Cayman Chemical

    A chemical chaperone that rescues the trafficking of misfolded proteins and weakly blocks HDAC activity (IC50 = 0.4 mM), leading to cell cycle arrest, differentiation, and/or apoptosis of various tumors.

  • AH 6809

    Cayman Chemical

    AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809 blocks the PGE2-induced accumulation of cAMP in COS cells transfected with the human EP2 receptor. It also blocks the accumulation of Ca2+ in Xenopus oocytes…

  • Etoposide

    Cayman Chemical

    An inhibitor of topoisomerase II (IC50 = 60.3 μM); can have much greater potencies when evaluated in cell-based cytotoxicity assays (e.g., IC50 = 5.14 nM for MCF-7 cells); can also inhibit nuclear receptor coactivator 3 (IC50 of 2.48 μM).

  • 4(Z),7(Z)-Decadienoic Acid-d5

    Cayman Chemical

    An internal standard for the quantification of 4(Z),7(Z)-decadienoic acid by GC- or LC-MS.

  • 4-bromo-A23187

    LKT Labs

    Non-fluorescent halogenated A23187 analog and Ca2+ ionophore. It induces formation of endothelial microvesicles, increasing leakage of lactate dehydrogenase and decreasing cell viability. It also induces mast cell degranulation and stimulates the acros

  • AZD-3463

    LKT Labs

    AZD-3463 is an inhibitor of anaplastic lymphoma kinase (ALK) and insulin-like growth factor 1 receptor (IGF-1R). This compound exhibits anticancer chemotherapeutic activity, inhibiting proliferation by altering downstream ERK/Akt/STAT3 signaling. AZD-3463 has induced regression or stasis in in vivo…

  • 4-Pyridylthioamide

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • Gilvocarcin V

    Cayman Chemical

    An antitumor antibiotic that inhibits DNA synthesis by promoting the selective cross-linking of both histone H3 and the heat shock protein, GRP78 to DNA when photoactivated by near-UV or visible light.

  • Propidium Iodide

    Cayman Chemical

    A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

  • Indole-3-thio Carboxamide

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • RITA

    Cayman Chemical

    An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

  • Cisplatin

    LKT Labs

    Cisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…

  • Acetaminophen

    Cayman Chemical

    An analgesic and antipyretic compound; inhibits COX-2 activity by more than 80%, albeit at relatively high doses, while it is less effective against COX-1.

  • FAK Inhibitor 14

    Cayman Chemical

    A direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 (IC50 = 1 μM); no known significant effect on the activity of a range of other kinases; promotes cell detachment and inhibits cell adhesion of cells in culture; blocks tumor growth in vivo.

  • 17-phenyl trinor Prostaglandin F2a methyl ester

    Cayman Chemical

    A lipophilic analog of 17-phenyl trinor PGF2α, a potent agonist for the FP receptor.

  • AK-7

    Cayman Chemical

    A cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM); dimishes neuronal cell death induced by mutant huntingtin fragment in culture; down-regulates cholesterol biosynthetic gene expression and reduces total cholesterol levels in neurons in vivo.

  • Acarbose

    Cayman Chemical

    An α-glucosidase inhibitor that delays the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase and sucrase (IC50s = 0.16 and 2.9 µM, respectively).

  • Acetylsalicylic Acid

    LKT Labs

    NSAID and COX-1/2 inhibitor used to decrease inflammation. It inhibits platelet aggregation and prolongs bleeding time by decreasing levels of thromboxane A2. Chronic administration decreases risk of cancer and cardiovascular events.

  • Abiraterone

    LKT Labs

    Progesterone derivative and Cyp17A1 inhibitor used to treat castration-resistant prostate cancer. It decreases androgen production and may inhibit eIF4F signaling.

  • NU 1025

    Cayman Chemical

    An inhibitor of PARPs (IC50 = 400 nM); enhances the cytotoxicity of γ-irradiation and certain anticancer drugs; also used to study the regulation of DNA repair by PARP enzymes.

  • CFDA-SE

    Cayman Chemical

    A stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.

  • Phosphine-biotin

    Cayman Chemical

    A labeling reagent that selectively reacts with azido groups on modified proteins through the Staudinger ligation reaction; can be used in common avidin-based biochemical techniques in whole cells or by blotting experiments following SDS-PAGE; has been used successfully in conjunction with Daz-1 or…

  • Amitriptyline Hydrochloride

    LKT Labs

    Amitriptyline exhibits antidepressant, antipsychotic, analgesic, and antinociceptive activities; it acts as an antagonist at 5-HT2A/2C/6/7 receptors, M1-5 muscarinic acetylcholine receptors (mAChRs), H1/4 histamine receptors, a1-adrenergic receptors, and also on the serotonin transporter (SERT) and…

  • 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.

  • Abacavir Sulfate

    LKT Labs

    Guanosine analog and inhibitor of RT, guanylyl cyclase, and telomerase used to treat HIV infection. Grade: ≥98%

  • Aflatoxin B1

    LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin B1 is the most cytotoxic of all aflatoxins; it inhibits DNA synthesis and induces cell cycle arrest.

  • A-779

    LKT Labs

    Mas antagonist that inhibits signaling by angiotensin (1-7), preventing vasodilation and insulin sensitization.

  • Bilirubin from Porcine Gall Bladder

    MP Biomedicals

    Bilirubin is the principal pigment of bile and constituent of many biliary calculi and also found in blood. As the major end-product of the biological breakdown of heme, bilirubin is the chromophore responsible for coloration in various forms of jaundice. Bilirubin is suitable for use in the…

  • Hydrocortisone

    MP Biomedicals

    Hydrocortisone, a primary glucocorticoid secreted by the adrenal cortex. It has three times the anti-inflammatory potency of corticosterone but much lower Na2+ retention potency. Hydrocortisone, known more formally as cortisone (INN, USAN, BAN), is a steroid hormone, produced by the zona…

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