Biologically Active Small Molecules

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LKT Labs Biologically Active Small Molecules

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  • 10-Hydroxycamptothecin

    LKT Labs

    10-Hydroxycamptothecin is a camptothecin derivative. Camptothecin is a quinolone alkaloid precursor of irinotecan; it is originally produced by Camptotheca. Camptothecin exhibits anticancer chemotherapeutic activity, inhibiting topoisomerase I and inducing double-stranded DNA breaks. Camptothecin…

  • 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…

  • Benzydamine Hydrochloride

    LKT Labs

    Benzydamine is a non-steroidal anti-inflammatory drug (NSAID) that also exhibits analgesic, anesthetic, and antibacterial activities. Benzydamine is clinically used to treat mucositis and sore throat. Unlike most NSAIDs, benzydamine inhibits prostaglandin synthetase, not cyclooxygenase (COX).

  • Calcitonin, chicken

    LKT Labs

    Calcitonin is an endogenous neuropeptide that exhibits pro-oncogenic, anti-osteoarthritic, and anti-resorptive activities. Calcitonin induces activation of NF-?B, upregulating expression and activity of fibronectin, MMP-1, MMP-2, and MMP-9 and increasing cell growth in osteosarcoma cells. When…

  • Carbenoxolone Disodium

    LKT Labs

    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…

  • Agomelatine

    LKT Labs

    Agomelatine is a melatonin MT1/2 receptor activator that also inhibits 5-HT2C receptors. Agomelatine displays antidepressant, anxiolytic, and hypnotic characteristics and is currently being examined as a marketable antidepressant. Agomelatine improves

  • 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.

  • Capsaicin, natural

    LKT Labs

    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…

  • Catch-Relaxing Peptide

    LKT Labs

    Catch-relaxing peptide (CARP) is a peptide originally found in mollusks that exhibits neuromodulatory and cardiomodulatory activity. CARP decreases heart rate and modulates muscle contractility in vivo. Additionally, CARP decreases slowly-inactivating Ca2+ and Ca2+-activated K+ currents in snail…

  • Brain Injury-derived Neurotrophic Peptide (3)

    LKT Labs

    This peptide supports neuronal survival and protects neurons in glutamate-induced cell death assays.

  • ß-Amyloid Peptide (1-42), rat

    LKT Labs

    Amyloid-ß (Aß) is a peptide cleavage product of amyloid precursor protein (APP) that is often used as a biomarker in Alzheimer’s disease. Misfolded Aß oligomers instigate conformation changes in other, normally folded Aß oligomers, increasing the number of misfolded proteins and eventually forming…

  • L-(+)-Alliin

    LKT Labs

    L-(+)-Alliin is a cysteine derivative originally found in Allium sativum (garlic); it exhibits anti-inflammatory, neuromodulatory, anti-diabetic, anti-hyperlipidemic, antioxidative, cardioprotective, and anti-angiogenic activities; it is the optically active and orally bioavailable isomer of…

  • A66

    LKT Labs

    Inhibitor of p110a PI3K. It decreases viability of endometrial cancer cells and impairs glucose and insulin tolerance.

  • Bis(aziridinyl)methylamino Phosphine Sulfide

    LKT Labs

    Bis(aziridinyl)methylaminophosphine is an anti-fertility/sterilization agent used to sterilize male insects and lamprey eels. This compound induces DNA fragmentation in spermatozoa and is very hazardous.

  • Busulfan

    LKT Labs

    Busulfan is an alkyl sulfonate that exhibits anticancer chemotherapeutic activity. Busulfan is an alkylating agent that attaches an alkyl group to the N7 position of guanine bases, inhibiting DNA replication; it is clinically used to treat chronic myelogenous leukemia (CML). In vitro, busulfan…

  • BI-6727

    LKT Labs

    BI-6727 is a polo-like kinase 1 (PLK1) inhibitor that exhibits anticancer activity. In vitro, BI-6727 induces apoptosis in acute myelogenous leukemia (AML) cells. This compound is currently in clinical trials as a potential treatment for several cancers; it improves response and survival rates.

  • Amiodarone Hydrochloride

    LKT Labs

    Amiodarone is a class III anti-arrhythmic that inhibits Na+ channels, voltage-gated Ca2+ channels, voltage-gated K+ channels, and a/ß-adrenergic receptors. Amiodarone prolongs the duration of the action potential, increasing the length of the refractory period; it is clinically used to treat…

  • AZD-6482

    LKT Labs

    AZD-6482 is an inhibitor of p110ß PI3K. AZD-6482 inhibits insulin-induced adipocyte glucose uptake in vitro and increases glucose homeostasis in vivo. Additionally, AZD-6482 exhibits antithrombotic activity without increasing bleeding time or blood loss in other animal models.

  • 3-Aminobenzamide

    LKT Labs

    3-Aminobenzamine is an inhibitor of poly(ADP)-ribosyl polymerase (PARP) that exhibits cytoprotective, anti-atherosclerotic, and anticancer activities. 3-Aminobenzamide prevents UV-induced cell death in vitro and inhibits TGF-ß1-induced phosphorylation of Smad3 in other cellular models. In vivo,…

  • 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…

  • CEF10

    LKT Labs

    CEF peptides are v-Src-induced cytokines from chicken embryo fibroblasts. These peptides are biomarkers of CEF transformation by Rous sarcoma virus. Grade: ≥95%

  • L-Alaninol

    LKT Labs

    L-Alaninol is an amino acid alcohol that exhibits anticancer activity. L-Alaninol inhibits proliferation of melanoma cells and increases levels of cytochrome c reductase and tau-glutamyl transpeptidase. Grade: ≥98%

  • Carcinoembryonic Antigen (605-613) analog

    LKT Labs

    This peptide is an epitope of carcinoembryonic antigen and is recognized by T cells in the immune system; it may have potential in the development of vaccines or targeting therapies. This analog differs slightly from the original peptide, with a N610D Grade: ≥95%

  • Azaperone

    LKT Labs

    Azaperone is a butyrophenone tranquilizer that exhibits sedative activity through the inhibition of a-adrenergic receptors. Azaperone also inhibits dopamine receptors and histamine receptors; it also may display antiemetic, antipsychotic, antihistaminergic, and anticholinergic activities.

  • Bradykinin Triacetate

    LKT Labs

    Bradykinin is a peptide that exhibits natriuretic, antioxidative, vasodilatory, and pro-angiogenic activities. Bradykinin stimulates bradykinin receptors and increases PLC activity, decreasing ENaC open probability, inhibiting distal nephron Na+ transport, and inducing natriuresis. In vitro,…

  • S-(-)-Carbidopa Monohydrate

    LKT Labs

    S-(-)-Carbidopa is a hydrazine that inhibits L-amino acid decarboxylase; it only acts peripherally when given systemically, as it does not cross the blood-brain barrier. S-(-)-Carbidopa inhibits formation of dopamine granules and dopamine-mediated swimming activity in sea urchins. In animal models…

  • Bis(salicyl) Fumarate

    LKT Labs

    Bis(salicyl) 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 anti-inflammatory,…

  • Azathioprine

    LKT Labs

    Azathioprine is a purine analog that acts as a prodrug of mercaptopurine. Azathioprine exhibits anticancer chemotherapeutic, immunosuppressive, and antiviral activities. Azathioprine inhibits amidophosphoribosyl transferase, inhibiting the production of adenine and guanine purines and preventing…

  • Caerulomycin A

    LKT Labs

    Caerulomycin A is a bipyridyl antifungal antibiotic. Caerulomycin A is toxic to Entamoeba in animal models of infection. Additionally, caerulomycin may exhibit anticancer and immunosuppressive activities. Grade: ≥96%

  • Cecropin B

    LKT Labs

    Cecropin B is an antimicrobial peptide (AMP) found in Hyalophora cecropia and Bombyx mori. Cecropin B exhibits antibacterial activity in vitro and in vivo against Haemophilus, Staphylococcus, and Escherichia. Grade: ≥95%

  • Butyric Acid Sodium

    LKT Labs

    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…

  • ABT-737

    LKT Labs

    BH3 mimetic and inhibitor of Bcl-2, Bcl-xl, and Bcl-w. It inhibits growth of acute myelogenous leukemia cells and induces apoptosis and clearance in platelets.

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