Biologically Active Small Molecules

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LKT Labs Biologically Active Small Molecules

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  • Cafestol Acetate

    LKT Labs

    Cafestol is a diterpene initially found in brewed, unfiltered coffee that exhibits anti-angiogenic, anticancer, chemopreventive, neuromodulatory, anti-inflammatory, and hyperlipidemic activities. Cafestol inhibits proliferation, migration, and tube formation in vitro, potentially through decreasing…

  • Benfotiamine

    LKT Labs

    Thiamine/vitamin B derivative and antioxidant. It displays several biological activities, including inhibiting pain neurotransmission, decreasing production of production of amyloid-β, and inhibiting LPS-induced release of leukotrienes, prostaglandins, and thromboxane B2.

  • AGDV

    LKT Labs

    AGDV is a C-terminal peptide sequence found on fibrinogen that is known as a binding site for glycoprotein IIb/IIIa (integrin aIIbß3); this binding is required for platelet adhesion and aggregation.

  • Azithromycin is an azalide macrolide antibiotic derived from erythromycin. Azithromycin binds the bacterial 50S ribosomal subunit, inhibiting protein translation. Azithromycin displays antibacterial, anti-fibrotic, and anti-inflammatory activities. In epithelial cells, azithromycin inhibits the…

  • Arformoterol is the R,R enantiomer of formoterol. Arformoterol exhibits anti-inflammatory and anti-asthma activities, potentiating the effects of co-administered glucocorticoids in the treatment of asthma and chronic obstructive pulmonary disorder (COPD). Arformoterol activates β2-adrenergic…

  • (+)-Bicuculline

    LKT Labs

    Bicuculline is a neuromodulatory GABA-A receptor antagonist used to study regional variation of GABA receptors and the role of GABA-A receptors in motor disorders, pain, seizure, nociception, anxiety, and memory. Through its inhibition of GABA-A receptors, bicuculline potentiates activation at NMDA…

  • Artemisinin

    LKT Labs

    Artemisinin is a sesquiterpene lactone originally found in Artemisia (wormwood); it is clinically used to treat malaria. Artemisinin exhibits anti-parasitic, antimalarial, cardioprotective, anticancer, and anti-inflammatory activities. This compound inhibits growth of Plasmodium. In animal models…

  • β-cembrenediol is a diterpene product found in tobacco plants and cigarette smoke. β-cembrenediol displays weak anticancer and antimicrobial activity, exhibiting some cytotoxicity in cellular models. Grade: ≥98%

  • Carvedilol

    LKT Labs

    Carvedilol is an a1- and ß1/2-adrenergic receptor antagonist used to treat congestive heart failure; its inhibitory action at adrenergic receptors slows heart rhythm, decreasing force, pressure, and cardiac workload. Carvedilol also inhibits release of pro-inflammatory cytokines TNF-a and…

  • 4-Bromoflavone

    LKT Labs

    4-Bromoflavone displays antioxidative and chemopreventive activities. 4-Bromoflavone activates Nrf2-Keap1-ARE complex signaling and also induces quinone reductase and other phase II enzymes. Additionally, this compound prevents the development of mammary tumors, increasing tumor latency in vivo.

  • Altrenogest

    LKT Labs

    Altrenogest is a progestogen used in veterinary settings. This progesterone agonist is most commonly used to suppress or control the estrous cycle of female animals.

  • Carbadox

    LKT Labs

    Carbadox is an antibiotic compound used to treat livestock; it exhibits antibacterial activity against Lawsonia and Treponema. Carbadox is also used as a growth promoter and may be mutagenic.

  • Carnosic Acid

    LKT Labs

    Carnosic acid is a diterpene found in Rosmarinus that exhibits antioxidative, anti-inflammatory, neuroprotective, cognition enhancing, and anticancer chemotherapeutic activities. Carnosic acid inhibits growth of colon adenocarcinoma cells and decreases tumor number in vivo by downregulating…

  • Calcitonin gene-related peptide (CGRP) is an endogenous neuropeptide that exhibits anti-inflammatory, anti-resorptive, anxiogenic, neuroprotective, and pro-angiogenic activities. In animal models of livery injury, CGRP displays protective benefit, decreasing pro-inflammatory cytokine levels. CGRP…

  • 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…

  • Canthaxanthin

    LKT Labs

    Canthaxanthin is a carotenoid terpene pigment initially found in various sources including plants and fish. Canthaxanthin exhibits immunostimulatory, antioxidative, and chemopreventive activities; it does not display any vitamin A activity. In vivo, canthaxanthin increases cell-mediated and humoral…

  • Auraptene

    LKT Labs

    Auraptene is a monoterpene coumarin originally found in Citrus species. Auraptene exhibits anti-inflammatory, neuroprotective, anti-parasitic, antihypertensive, anti-diabetic, and chemopreventive activities. Auraptene inhibits growth of species of Leishmania, decreases mean arterial pressure, binds…

  • Balofloxacin is a fluoroquinolone antibiotic that displays strong antibacterial activity against gram-positive bacteria and weak antibacterial activity against gram-negative bacteria. Balofloxacin inhibits the supercoiling ability of bacterial DNA gyrase, and shows efficacy treating early and…

  • 3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…

  • TRPA1 channel agonist and xanthine oxidase inhibitor. It increases levels of phase II enzymes in models of colon carcinogenesis and suppresses tumor growth in animal models of squamous cell carcinoma. In other cancer models, it prevents angiogenesis an

  • Asperosaponin VI

    LKT Labs

    AS-703026 is an inhibitor of MEK1/2 that exhibits anticancer chemotherapeutic activity. In vitro, AS-703026 inhibits proliferation of melanoma cells. In both in vitro and in vivo models of colorectal cancer containing WT Ras or mutant KRAS, AS-703026 inhibits growth of cells and also of tumors.…

  • Angiotensin II (AT II) is a peptide produced from AT I by angiotensin-converting-enzyme (ACE). AT II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca2+ levels; this results in contraction and vasoconstriction, increasing blood…

  • Amphotericin B

    LKT Labs

    Amphotericin B is a polyene antifungal compound that increases levels of ROS and forms pores or channels in membranes by binding membrane sterols. Amphotericin B induces iNOS, activates astrocytes, and increases expression of IL-1ß, TNF-a, BDNF, and GDNF, displaying potential neuroprotective…

  • Carbenoxolone

    LKT Labs

    Carbenoxolone is a synthetic derivative of the active component of licorice (Glycyrrhiza glabra) and is most well known for its ability to inhibit gap junction connexin channels and 11ß-hydroxysteroid dehydrogenase. Carbenoxolone displays a wide variety of beneficial properties, including…

  • 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.

  • Chondroitin sulfate (CS) is a polyanionic sulfated glycosaminoglycan that displays anti-arthritic, antioxidative, and anti-inflammatory activities. CS is an endogenous component of the extracellular matrix of connective tissues and is responsible for their resistance and elasticity. CS is often…

  • Ciprofibrate

    LKT Labs

    Ciprofibrate is a PPARa agonist that exhibits anti-hyperlipidemic activity. Clinically, ciprofibrate decreases levels of triglycerides and total cholesterol and increases levels of HDL. In hepatoma cells, ciprofibrate increases NF-?B DNA binding activity. Additionally, ciprofibrate induces…

  • 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.

  • Caspofungin acetate is a lipopeptide antifungal that inhibits the enzyme 1,3-ß-Glucan synthase, which synthesizes ß-glucan polymers that form fungal cell walls. Caspofungin acetate is active against a variety of Aspergillus and Candida species and unlike many antifungals, is not metabolized by the…

  • (+)-Catechin

    LKT Labs

    Catechin is a flavanol originally found in Camilla and other plant sources; it exhibits antioxidative, anti-aging, anti-atherosclerotic, anti-ulcerative, neuroprotective, neuromodulatory, anticancer chemotherapeutic, and chemopreventive activities. Catechin increases life span in Caenorhabditis…

  • 6-Aminocaproic acid is a protease inhibitor that displays anticancer activity but is limited by cytotoxicity. 6-Aminocaproic acid inhibits plasmin, preventing fibrinolysis; it may exhibit pro-thrombotic activity, as it is clinically used to treat bleeding disorders.

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

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