1 mg, Biologically Active Small Molecules

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  • Cayman Chemical

    A selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.

  • Cayman Chemical

    A PARP1 inhibitor (IC50 = 450 nM) that displays neuroprotective effects in cultured mouse cortical neurons; also inhibits eosinophilic infiltration into airways of OVA-challenged mice and induces the regression of atherosclerotic plaques in high-fat fed ApoE(-/-) mice.

  • Cayman Chemical

    A selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).

  • Cayman Chemical

    A pan inhibitor PKD (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively); blocks cell proliferation, induces apoptosis, and reduces the viability of pancreatic cancer cells both in vitro and in vivo.

  • Cayman Chemical

    A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO3- secretion in the stomach.

  • Cayman Chemical

    A potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.

  • Cayman Chemical

    A natural sesquiterpene lactone that reduces growth (EC50 = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC50 = 10 μM); inhibits telomerase…

  • Cayman Chemical

    A reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).

  • Cayman Chemical

    A stable and efficient hole-transport material in organic light-emitting devices and in ssDSSCs; yields high ssDSSC efficiency due to its excellent pore-filling property into mesoporous titania films.

  • Cayman Chemical

    A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

  • Cayman Chemical

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

  • Cayman Chemical

    An analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.

  • Cayman Chemical

    A cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…

  • Cayman Chemical

    A specific inhibitor of N-linked glycoslylation that blocks the first step of glycoprotein synthesis and induces protein unfolding; impairs the function of several receptor tyrosine kinases, including EGFR, ErbB2, ErbB3, IGF-IR, and ALK; radiosensitizes glioma and pancreatic adenocarcinoma cells to…

  • Cayman Chemical

    A membrane-permeant, fluorescent Na+ indicator dye; increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.

  • Cayman Chemical

    A small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

  • Cayman Chemical

    IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor that demonstrates IC50 values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively. It is inactive against tryptophan 2,3-dioxygenase (TOD; IC50 > 10 µM).

  • Cayman Chemical

    A natural yellow carotenoid, which can be found in plants, egg yolks, and in the human retina; a lipid-soluble antioxidant that can circulate in the plasma and confer cardioprotective, anti-inflammatory, and anti-angiogenic effects.

  • Cayman Chemical

    Inhibits calcium/calmodulin-dependent phosphodiesterase from bovine brain, presumably PDE1 (IC50 = 15 mM).

  • Selectively and competitively blocks T3 binding to both TRα and TRβ (IC50s = 1.5 µM), demonstrating ~1000-fold lower affinity for TRα in intact cells compared with T3.

  • Cayman Chemical

    A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.

  • Cayman Chemical

    A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM).

  • Cayman Chemical

    A potent antagonist for the human IP (prostacyclin) receptor that antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cAMP accumulation in a dose-dependent manner; inhibits the binding of tritiated iloprost to rodent neuroblastoma cells (Ki = ~ 3 nM).

  • 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.

  • Cayman Chemical

    A cell-permeable mycotoxin which binds to the barbed end of actin, reversibly inhibiting the elongation and shortening of actin filaments; blocks diverse cellular functions, including cell division, migration, phagocytosis, exocytosis, chemotaxis, and glucose transport.

  • Cayman Chemical

    A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

  • PGF2α 1,15-lactone is a lipid-soluble internal ester of PGF2α. Hydrolysis of the lactone readily produces free PGF2α in plasma. In rhesus monkeys, a total dose of 15 mg of PGF2α 1,15-lactone terminates early pregnancy, whereas PGF2α is ineffective.

  • Cayman Chemical

    A selective inhibitor of class IIa HDACs, with greater than 170-fold selectivity over class I HDACs, including HDAC1; used in cells (1-10 µM) and in mice to elucidate the roles of class IIa HDACs in cell proliferation and differentiation, apoptosis, myogenesis, adipogenesis, and fibrosis.

  • Cayman Chemical

    A fluorogenic substrate that can be cleaved specifically by group I caspases.

  • Cayman Chemical

    ICI 192605 is a potent antagonist of the thromboxane A2 receptor (TP) that blocks contraction of isolated guinea pig trachea induced by U-46619 (Item No. 16450; Kd = 0.398 nM). It is used to study the role of TP signaling in tissues and animals.

  • O-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a…

  • Cayman Chemical

    6-keto prostaglandin F (6-keto PGF) is the inactive, non-enzymatic hydrolysis product of PGI2. 6-keto PGF serves as a useful marker of PGI2 biosynthesis in vivo. When [ 3 H]-PGI2 is injected into healthy human…

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