Biologically Active Small Molecules

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LKT Labs Biologically Active Small Molecules

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  • Chlorpheniramine is a first generation alkylamine antihistamine that inhibits H1 histamine receptors, serotonin transporters (SERT), and norepinephrine transporters (NET); it exhibits anti-allergic and antidepressant activities. Chlorpheniramine is clinically used to treat allergic rhinitis and…

  • Abacavir

    LKT Labs

    Guanosine analog and inhibitor of RT, guanylyl cyclase, and telomerase used to treat HIV infection.

  • Cantharidin

    LKT Labs

    Canthardin is a toxin initially produced by the blister beetle, Canarthis vesicatoria. Canthardin competitively inhibits serine/threonine phosphatases such as protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A). Canthardin exhibits anticancer and anti-resorptive activities. In cancer…

  • Capsaicin is an agonist of transient receptor potential vanilloid (TRPV) channels that was originally found in peppers of the Capsicum genus. Capsaicin exhibits analgesic, anti-inflammatory, anti-obesity, and anticancer chemotherapeutic activity. Capsaicin also displays bronchoconstrictive activity…

  • Actinomycin

    LKT Labs

    Actinomycin D is a polypeptide antibiotic produced from Streptomyces; it exhibits anticancer chemotherapeutic activity but does not display antibacterial benefit. Actinomycin D is clinically used to treat various cancers and is one component of the VAC chemotherapy regimen. Actinomycin D binds DNA,…

  • Bis(3,5-dibromosalicyl) fumarate is an aspirin analog that is used to induce hemoglobin chain crosslinks at lysine residues. This compound is used to study hemoglobin function in research models and may be used to develop treatments for sickle-cell anemia. This compound may exhibit…

  • Artesunate

    LKT Labs

    Artesunate is a sesquiterpene lactone derived from Artemisia. Artesunate exhibits anticancer chemotherapeutic, antiviral, anti-angiogenic, and anti-parasitic activities. Artemisinins such as artesunate are best known for their antimalarial activity. Artesunate induces G0/G1 phase cell cycle arrest,…

  • Calcitriol

    LKT Labs

    Calcitriol is the active form of vitamin D that binds to the vitamin D receptors (VDR), increasing absorption of dietary Ca2+. Calcitriol is produced in the kidney from prodrug forms of vitamin D such as cholecalciferol. Calcitriol is commercially used in dietary supplements to prevent…

  • Cefotaxime is a third generation β-lactam cephalosporin antibiotic. Cefotaxime exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding proteins to prevent peptidoglycan synthesis and bacterial cell wall formation. Cefotaxime is also…

  • A-779

    LKT Labs

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

  • Aflatoxin M1

    LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M1 is the hydroxylated metabolite of aflatoxin B1; it inhibits DNA synthesis and induces cell cycle arrest.

  • Cambinol

    LKT Labs

    Cambinol is an inhibitor of sirtuins, particularly sirtuin1. Cambinol exhibits anti-inflammatory and anticancer chemotherapeutic activities. In various cell lines, cambinol suppresses MAPK and MEK signaling and inhibits expression of pro-inflammatory cytokines such as IL-1ß, IL-6, TNF-a, and…

  • Carbamazepine

    LKT Labs

    Carbamazepine is an antiepileptic/anticonvulsant that also exhibits antipsychotic and anti-inflammatory activities. Carbamazepine inhibits voltage-gated Na+ channels, stabilizing the inactive conformation of the channel. Carbamazepine also potentiates GABA receptor signaling and inhibits…

  • Ambroxol is a bronchial expectorant that also exhibits antioxidative activity. Ambroxol stimulates the ciliary beat frequency and increases mucous secretion in the lung and trachea. In clinical settings, ambroxol increases levels of thioredoxin and thioredoxin reductase, decreasing oxidative stress…

  • Berberine is an isoquinoline alkaloid found in a variety of plants, including barberry, goldenseal, Oregon grape, California poppy, and the Amur cork tree. Berberine fluoresces under ultraviolet light and is often used to stain heparin in mast cells. Berberine displays many beneficial effects,…

  • Chlortetracycline is a tetracycline antibiotic that also exhibits antioxidative, anti-parasitic, and neuroprotective activities. Chlortetracycline binds the 30S subunit of the bacterial ribosome, inhibiting protein synthesis; it also displays antibacterial and antimalarial properties. Additionally,…

  • BMS-911543

    LKT Labs

    BMS-911543 is an oral selective inhibitor of JAK2 currently in clinical trials. BMS-911543 shows anticancer activity through inhibition of the JAK/STAT signaling cascade in in vitro and in vivo models of myeloproliferative neoplasms, which display constitutively active JAK2 signaling. This compound…

  • BKM120

    LKT Labs

    BKM120 is an inhibitor of PI3K that is currently in clinical trials as a potential treatment for brain metastases of HER2+ breast cancer and other solid tumors. BKM120 exhibits anticancer chemotherapeutic and anti-metastatic activities, inducing G2/M phase cell cycle arrest, polyploidy, and…

  • 7-Aminoactinomycin D (7AAD) binds DNA sequences and is used in cellular assays to measure apoptosis and phagocytosis.

  • Aspartame

    LKT Labs

    Aspartame is a dipeptide ester that is used as an artificial sweetener in commercial food production. Aspartame exhibits antibacterial efficacy against Porphyromonas, a periodontal pathogen. In vivo, aspartame also displays antinociceptive activity, increasing latency times in tail flick and paw…

  • Biotin

    LKT Labs

    Biotin is a water-soluble B vitamin (vitamin B7) that may be found in many foods but is also administered as a dietary supplement. Biotin is a coenzyme involved in the synthesis of fatty acids, isoleucine, and valine; it also plays a role in gluconeogenesis. Biotin may be found attached to lysine…

  • Bleomycin A5 is an anticancer chemotherapeutic that binds DNA and induces DNA cleavage and strand breaks; it is highly toxic. Bleomycin is clinically used to treat lymphomas, squamous cell carcinomas, and testicular cancer. Additionally, this compound induces apoptosis, alters cell cycle…

  • Cetrimide

    LKT Labs

    Cetrimide is a mix of quaternary ammonium salts that exhibits antiseptic and anticancer chemotherapeutic activities. Cetrimide acts as a cationic detergent, altering the mitochondrial membrane potential and inducing pore formation in membranes. Cetrimide bromide inhibits H+ ATP synthase, inducing…

  • Dihydroartemisinin is a sesquiterpene lactone that can be derived from Artemisia. Dihydroartemisinin exhibits anticancer, antiviral, anti-inflammatory, anti-asthma, and anti-parasitic activities. Artemisinins such as dihydroartemisinin are best known for their antimalarial activity.…

  • Arvanil

    LKT Labs

    Arvanil is an agonist at transient receptor potential vanilloid 1 (TRPV1) channels and cannabinoid 1 (CB1) receptors. Arvanil exhibits antidepressant, hypertensive, immunosuppressive, anti-inflammatory, antiemetic, and anticancer activities. Arvanil decreases immobility time in vivo in the forced…

  • 2-Tert-butyl-4-hydroxyanisole (2-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative activity. 2-BHA acts as a phase II enzyme inducer, increasing levels of glutathione and glutathione-S-transferase.

  • Betulinic Acid

    LKT Labs

    Betulinic acid is a pentacyclic triterpene that exhibits antithrombotic, anti-atherosclerotic, antioxidative, anti-inflammatory, anti-angiogenic, and anticancer chemotherapeutic properties. Betulinic acid decreases expression of P-selectin and binding of PAC-1, preventing platelet aggregation. In…

  • This compound is a conjugate of N-acetyl-cysteine and sulforaphane. Like other isothiocyanates (ITCs), this compound likely displays antioxidative activity. Grade: ≥98%

  • Sodium butyrate is an inhibitor of histone deacetylases (HDACs) that exhibits antidepressant, immunomodulatory, and anticancer activities. In animals undergoing the light dark test, tail suspension test, and forced swim test, sodium butyrate decreases restraint stress-induced depression. In…

  • Adipokinetic hormone is a neuropeptide hormone found in insects that is involved in the regulation of circadian rhythms. Adipokinetic hormone also increases activity of peptidase, lipase, amylase, and polygalacturonase in the salivary glands. In brain samples treated with H2O2, this peptide…

  • N-acetyl-D-leucine is a D-amino acid that is deacylated in bacteria by d-aminoacylase enzymes. D-amino acids inhibit bacterial biofilm formation when they are incorporated into the cell wall. Compounds such as N-acetyl-D-leucine induce release of amyloid fibers that link cells together in the…

  • Adenine

    LKT Labs

    Adenine is a purine nucleotide base that is involved in the synthesis of RNA and DNA. Adenine also plays roles in cellular respiration as a component of ATP, NAD, and FAD. Grade: ≥98%

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