Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • L-NAME (hydrochloride)

    Cayman Chemical

    A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

  • Guaiacol

    Cayman Chemical

    Guaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of COX enzymes. It can therefore serve as a reducing co-substrate for COX reactions. The one-electron oxidation…

  • CAY10591

    Cayman Chemical

    An activator of SIRT1 that decreases TNF-α levels from 325 pg/ml (control) to 104 and 53 pg/ml at 20 and 60 µM, respectively; exhibits a significant dose-dependent effect on fat mobilization in differentiated adipocytes.

  • BSI-201

    Cayman Chemical

    An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

  • SU 9516

    Cayman Chemical

    A potent inhibitor of several CDKs with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.

  • Produced by selective hydrolysis of the terminal saccharide unit of ivermectin; inhibits nematode larval development.

  • A muscarinic M1 and M2 mACh receptor agonist (pKB = 5 and 3.7, respectively) that is typically used as an animal model for temporal lobe epilepsy.

  • Phenolic compounds, particularly flavonoids, from plant sources have long been observed to have antioxidant activity with potential benefits for human health. EGCG is a principle phenolic antioxidant found in a variety of plants, including green and black tea. EGCG inhibits cellular oxidation of…

  • Dithranol

    MP Biomedicals

    Dithranol (1, 8 - dihydroxy-9-anthrone) is also called as anthralin. It is a vital topical antipsoriatic drugs. Dithranol, an athracene derivative, is a free radical generating mitochondrial poison that induces apoptosis in keratinocytes. Dithranol may be used as a matrix for matrix assisted…

  • N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-4AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.1 and 0.625 µM, respectively. It is about 80 times less potent as an inhibitor of…

  • A nucleotide that upon phosphorylation to GTP becomes incorporated into RNA; used to study modulation of glutamatergic neurotransmission.

  • Bleomycin (sulfate)

    Cayman Chemical

    A glycopeptide antitumor antibiotic that produces single and double-strand DNA breaks in tumor cells to interrupt their cell cycle; has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models…

  • GSK2334470

    Cayman Chemical

    A selective PDK1 inhibitor (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members; suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well…

  • 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…

  • Tetrazolium (chloride)

    Cayman Chemical

    A redox indicator used to detect cellular respiration; primarily reduced by Complex I in mitochondria and, under anaerobic conditions, is completely reduced to an insoluble red 1,3,5-triphenylformazan.

  • Both inhibits and inactivates, at 100 µM, certain microsomal CYP450 enzymes (CYP2E1 and CYP2B4), but not others (CYP1A2).

  • Chloroquine (phosphate)

    Cayman Chemical

    An aminoquinoline antimalarial compound that is widely used as an autophagy inhibitor, preventing autophagosome fusion with lysosomes and inhibiting lysosomal acidification.

  • WYE-354

    Cayman Chemical

    A selective, potent, and cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

  • Asiaticoside

    LKT Labs

    Asiaticoside is a triterpene found in Centella that exhibits anti-inflammatory, neuroprotective, cognition enhancing, antipyretic, antioxidative, pro-angiogenic, anticancer chemotherapeutic, and chemopreventive activities. Asiaticoside inhibits melanogenesis by decreasing DNA binding by MITF; as a…

  • Green CMFDA

    Cayman Chemical

    A cell-permeable fluorescent probe that freely enters living cells, where it is transformed into a cell-impermeable, soluble, fluorescent compound; does not affect cell viability or proliferation and stably fluoresces for at least 72 hours, allowing for its use in cell tracking.

  • 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…

  • NU 7441

    Cayman Chemical

    A selective DNA-PK inhibitor (IC50 = 14 nM) that increases the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and potentiates the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

  • Tris-HCl Stock Solution (1 M, pH 7.5) contains filtered Tris-HCl (1 M, pH 7.5). It is ready to use as supplied.

  • Syringic Acid

    Cayman Chemical

    A naturally occurring O-methylated phenolic acid that can be enzymatically degraded by some bacteria as a source of methane or methanol; inhibits aldose reductase (IC50 = 213 µg/ml), proteasome activity, and cancer cell proliferation.

  • An alkaline aluminum−sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury; inhibits thrombin activity (IC50 = 4.5 µM) and prevents FGF-2 binding to endothelial cells, inhibiting tumor growth in mouse…

  • Paclitaxel

    Cayman Chemical

    A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

  • Prostaglandin D1 Alcohol

    Cayman Chemical

    A synthetic analog of PGD1 with a hydroxyl-group in place of the C-1 carboxylic acid.

  • 4-bromo-A23187

    LKT Labs

    Non-fluorescent halogenated A23187 analog and Ca2+ ionophore. It induces formation of endothelial microvesicles, increasing leakage of lactate dehydrogenase and decreasing cell viability. It also induces mast cell degranulation and stimulates the acros

  • Ac-YVAD-CMK

    Cayman Chemical

    A selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.

  • ZM 447439

    Cayman Chemical

    A selective inhibitor of Aurora B kinase (IC50 = 10 µM), less potently inhibiting Aurora C and A (IC50 = 250 and 1,000 nM, respectively); has been used to study the role of Aurora B in molecular events associated with mitosis and cytokinesis; selectively inhibits…

  • DL-a-Lipoic Acid

    Cayman Chemical

    DL-α-lipoic acid is a cyclic disulfide antioxidant that interconverts with its reduced dithiol form. It is an essential cofactor for decarboxylation reactions of the citric acid cycle, and acts as a general antioxidant.{12280,12281,12322} DL-α-lipoic acid can act as a direct radical…

  • Letermovir

    Cayman Chemical

    A small molecule inhibitor of human cytomegalovirus viral replication (EC50 = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

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