Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    An internal standard for the quantification of DHA by GC- or LC-MS.

  • A chromogenic substrate for endoglucanases and cellobiohydrolases.

  • LKT Labs

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

  • 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,…

  • Cayman Chemical

    An inhibitor of Cdc7 kinase (IC50 = 10 nM) as well as Cdk9, (IC50 = 34 nM); induces apoptotic cell death in multiple cancer cell types at 10 µM.

  • Cayman Chemical

    A naturally occurring electron donor for eight different enzymes, including those related to collagen hydroxylation, carnitine synthesis (which aids in the generation of ATP), norepinephrine synthesis, tyrosine metabolism, and amidating peptides.

  • Cayman Chemical

    A natural anthocyanin that has neuroprotective effects, reducing amyloid β-induced cytotoxicity in Neuro-2A cells; stimulates autophagy in U2OS cells.

  • Cayman Chemical

    A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC50 = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC25 = 0.45 nM); attenuates β-amyloid…

  • Cayman Chemical

    A platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC50 = 2 µM), blocking protein splicing and cell growth.

  • Cayman Chemical

    A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.

  • Cayman Chemical

    A potent PR and GR antagonist with Ki value of approximately 1 nM.

  • LKT Labs

    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.…

  • Cayman Chemical

    A dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A1, A2A, and A3 receptors with Ki values of 8.96, 23.0, and 8.3 µM, respectively.

  • LKT Labs

    Cholesterol is a sterol component of animal cell membranes that is required for membrane fluidity. Cholesterol is also the precursor to most steroid hormones, bile acids, and vitamin D compounds. Additionally, cholesterol is involved in vesicular transport and nerve conduction, and shows some…

  • Cayman Chemical

    A stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis by cytoplasmic esterases; used in experiments to increase levels of intracellular α-ketoglutarate and modulate a variety of enzymes, particularly in the context of glycolysis, hypoxia, and cancer.

  • LKT Labs

    Bifonazole is an imidazole antifungal that also exhibits anticancer activity. Bifonazole inhibits calmodulin, HMG-CoA reductase, and 14-a demethylase in fungi such as dermatophytes. Bifonazole also decreases cell viability and induces Ca2+-dependent apoptosis in prostate cancer cells and melanoma cells.

  • LKT Labs

    Aminopterin is a folic acid analog and derivative of pterin; it is very similar to methotrexate in structure. Aminopterin exhibits anticancer chemotherapeutic and immunosuppressive activities. Like other folic acid analogs, aminopterin inhibits dihydrofolate reductase, depleting nucleotide pools…

  • LKT Labs

    C59 is a PORCN inhibitor that exhibits anticancer chemotherapeutic activity, inhibiting the progression of mammary tumors in vivo by downregulating Wnt signaling. Grade: ≥98%

  • A mixture of trans (3R/7R and 3S/7S) isomers; induces the synthesis of proteinase inhibitors in plant leaves; in cancer cells, suppresses proliferation and induces apoptosis; inhibits hexokinase that is bound to mitochondria; methyl jasmonate derivatives also have potential as anti-inflammatory agents.

  • Cayman Chemical

    A physiologically active metabolite of losartan; a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.

  • Cayman Chemical

    A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.

  • 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…

  • Cayman Chemical

    A hybrid molecule patterned after N-arachidonoyl serotonin; inhibits capsaicin-induced TRPV1 channel activation (IC50 = 2.57 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC50 > 50 μM).

  • Cayman Chemical

    A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC50 = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.

  • Cayman Chemical

    A glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively); reversibly inhibits γ-glutamyl transpeptidase.

  • Cayman Chemical

    A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

  • Cayman Chemical

    An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC50 value of 15-25 µM.

  • Clodronate is a first-generation non-nitrogen-containing bisphosphonate that is used clinically for its anti-resorptive activity. Clodronate generates formation of a non-hydrolysable ß-? ATP analog that inhibits mitochondrial ADP/ATP translocase and prevents mitochondrial oxygen consumption…

  • Cayman Chemical

    An analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.

  • Cayman Chemical

    A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

  • N-(4-Carbethoxyphenyl)retinamide is a retinoid that exhibits anticancer chemotherapeutic and chemopreventive activities. This compound inhibits development of stomach and oral cancers in vivo and shows some benefit in the treatment of dysplasias. Additionally, this compound induces differentiation…

  • LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G1 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

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