1 mg, Biologically Active Small Molecules
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WH-4-023
Cayman ChemicalA 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.
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TIQ-A
Cayman ChemicalA 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.
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MLCK Inhibitor Peptide 18
Cayman ChemicalA selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).
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CRT0066101 (hydrochloride)
Cayman ChemicalA 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.
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ONO-8711
Cayman ChemicalA 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.
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Tetrodotoxin
Cayman ChemicalA 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.
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Costunolide
Cayman ChemicalA 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…
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cis-ACCP
Cayman ChemicalA 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).
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Spiro-MeOTAD
Cayman ChemicalA 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.
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Bafilomycin A1
Cayman ChemicalA 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.
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Nullscript
Cayman ChemicalAn analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.
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5-fluoro 203
Cayman ChemicalA 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,…
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Tunicamycin
Cayman ChemicalA 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…
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SBFI AM
Cayman ChemicalA 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.
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XAV939
Cayman ChemicalA 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.
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IDO-IN-1
Cayman ChemicalIDO-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).
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Lutein
Cayman ChemicalA 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.
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Obscurolide A1
Cayman ChemicalInhibits calcium/calmodulin-dependent phosphodiesterase from bovine brain, presumably PDE1 (IC50 = 15 mM).
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Thyroid Hormone Receptor Antagonist (1-850)
Cayman ChemicalSelectively 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.
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GDC-0152
Cayman ChemicalA 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.
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Tivantinib
Cayman ChemicalA 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).
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CAY10449
Cayman ChemicalA 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).
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Green CMFDA
Cayman ChemicalA 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.
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Cytochalasin B
Cayman ChemicalA 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.
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Ochratoxin A
Cayman ChemicalA 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,…
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Prostaglandin F2a 1,15-lactone
Cayman ChemicalPGF2α 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.
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MC 1568
Cayman ChemicalA 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.
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Ac-WEHD-AFC
Cayman ChemicalA fluorogenic substrate that can be cleaved specifically by group I caspases.
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ICI 192605
Cayman ChemicalICI 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.
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O-Acetyl Salicylhydroxamic Acid
Cayman ChemicalO-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…
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6-keto Prostaglandin F1a
Cayman Chemical6-keto prostaglandin F1α (6-keto PGF1α) is the inactive, non-enzymatic hydrolysis product of PGI2. 6-keto PGF1α serves as a useful marker of PGI2 biosynthesis in vivo. When [ 3 H]-PGI2 is injected into healthy human…