LKT Labs Biologically Active Small Molecules

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LKT Labs Biologically Active Small Molecules

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  • Alloxan is an oxygenated pyrimidine and toxic analog of glucose. Alloxan destroys ß cells and is used in research models to induce diabetes. This compound does not affect human cells.

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    Atriopeptin III is an analog of atrial natriuretic peptide (ANP) that exhibits vasodilatory/hypotensive and diuretic activities. In rat kidneys, atriopeptin III increases the diameter of constricted afferent arterioles, decreasing blood pressure.

  • Adrenocorticotropic hormone (ACTH) is a peptide derived from proopiomelanocortin (POMC) processed and secreted in the pituitary gland. ACTH binds and activates melanocortin-2 (MC2) receptors, stimulating cortisol production in the adrenal cortex. ACTH exhibits anti-inflammatory and immunomodulatory…

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    Antimycin A was initially produced by Streptomyces. Antimycin A binds cytochrome c reductase, inhibiting electron transport chain activity, oxidative phosphorylation, and ATP synthesis. Antimycin A is used in research models to study mitochondrial respiration and superoxide production. Grade: ≥98%

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

  • 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…

  • Ciclopirox is a hydroxypyridone compound that exhibits antifungal, anti-inflammatory, anti-angiogenic, and anticancer chemotherapeutic activities. This compound acts as a metal ion chelator, preventing peroxide degradation. Ciclopirox modulates generation of ROS in a PKA/Ras1/Ras2-dependent manner,…

  • Catharanthine is an alkaloid found in Catharanthus that is a chemical precursor in the synthesis of vinca alkaloids such as vinblastine and vincristine. Catharanthine displays weak anti-mitotic activity, binding tubulin poorly. Catharanthine exhibits anti-parasitic, vasodilatory, and…

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    AK-7 is an inhibitor of sirtuin 2 (SIRT2); sirtuins are considered class III histone deacetylases (HDACs). AK-7 exhibits neuroprotective activity, decreasing brain atrophy and improving motor function and survival in animal models of Huntington’s disea

  • Angiotensin I (AT I) is a peptide cleavage product of angiotensin and served no primary biological purpose other than to function as a precursor to angiotensin II.

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    CH5132799 is an inhibitor of PI3K that is somewhat selective for p110a isoforms. This compound exhibits anticancer chemotherapeutic activity, inhibiting cell proliferation and tumor growth in breast cancer, ovarian cancer, prostate cancer, and endometrial cancer models.

  • Carbenoxolone is a synthetic derivative of glycyrrhizin that exhibits anti-ulcerative, anti-inflammatory, neuromodulatory, neuroprotective, anti-hyperlipidemic, hepatoprotective, and immunosuppressive activities. Carbenoxolone is clinically used to treat ulcers and inflammation; it inhibits…

  • 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.

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    Acivicin is a fermentation product of Streptomyces; it is a glutamine analog. Acivicin inhibits ?-glutamyl transferase, CTP synthetase, GMP synthetase, and FGAM synthetase, preventing purine synthesis. Acivicin exhibits anticancer and antifungal activity, although its potential chemotherapeutic…

  • Anethole trithione is an oltipraz analog that is clinically used to treat xerostomia (dry mouth). Anethole trithione enhances salivary gland secretion.

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    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.

  • Chenodeoxycholic acid is an endogenous bile acid synthesized by the liver; it acts as an agonist at the farnesoid X receptor (FXR). Chenodeoxycholic acid exhibits anticancer and gastrointestinal motility modulating activities. This compound treats chronic constipation and displays protective…

  • 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,…

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    Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) that inhibits COX-2; it exhibits anti-inflammatory, analgesic, anticancer, and anti-metastatic activities. Celecoxib is clinically used to treat arthritis, acute pain, and ankylosing spondylitis. In hepatoma cells, celecoxib decreases the…

  • Mechlorethamine is a nitrogen mustard DNA alkylator that binds and alkylates the N7 nitrogen on guanine and adenine bases in DNA. Mechlorethamine was initially developed as a blistering agent for use in chemical warfare but has since exhibited anticancer chemotherapeutic benefit. In vitro and in…

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    Aceclofenac is a diclofenac analog that exhibits anti-inflammatory and analgesic activities. Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) that somewhat selectively inhibits COX-2; it is clinically used to treat rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.…

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    Cilostazol is a quinolone inhibitor of phosphodiesterase 3B (PDE 3B) that exhibits vasodilatory, antiplatelet, anti-inflammatory, anti-diabetic, antidepressant, anxiolytic, and pro-angiogenic activities. Cilostazol is clinically used to treat intermittent claudication associated with peripheral…

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    Bromosporine is an inhibitor of BET bromodomains (BRDs) BRD2, BRD4, BRD9, and CECR2; it may exhibit anticancer potential.

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    Cholecalciferol (vitamin D3) is an endogenous prodrug of calcifediol; cholecalciferol is synthesized in the skin under UV-B exposure. Cholecalciferol supplements are occasionally used to prevent bone loss. D vitamins commonly exhibit anti-osteoporotic, immunomodulatory, anti-inflammatory, 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…

  • Carvedilol phosphate is a cardioprotective a1- and ß1/2-adrenergic receptor inhibitor used to treat congestive heart failure; its inhibitory action at adrenergic receptors slows heart rhythm, decreasing force, pressure, and cardiac workload. Carvedilol phosphate also inhibits release of…

  • Besifloxacin is a fourth generation fluoroquinolone antibiotic that displays broad-spectrum antibacterial activity against aerobic and anaerobic bacteria and is effective against a wide range of ocular pathogens that exhibit resistance to other fluoroquinolone antibiotics. Besifloxacin inhibits DNA…

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    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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    Astilbin is a flavonoid found in several plants, including species of Engelhardia and Smilax. Astilbin displays anticancer, antioxidative, anti-inflammatory, and immunosuppressive activities. In vitro, astilbin inhibits expression of IL-1ß, IL-6, IL-10, MCP-1, and TNF-a, as well as activity of…

  • N-Acetyl-S-(N’-phenylthiocarbamoyl)-L-cysteine (PITC) is a cysteine conjugate of N-acetyl-phenylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer…

  • 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.

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