Biologically Active Small Molecules, 1 mg
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15(R)-17-phenyl trinor Prostaglandin F2a
Cayman ChemicalAn isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.
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SB-525334
Cayman ChemicalA potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.
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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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ML-324
Cayman ChemicalA cell-permeable inhibitor of JMJD2E (KDM4DL; IC50 = 920 nM); reduces the expression of immediate early genes of HSV (IC50 = ~10 µM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice.
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(R)-Butaprost
Cayman ChemicalButaprost is a structural analog of PGE2 with good selectivity for the EP2 receptor subtype. Butaprost has frequently been used to pharmacologically define the EP receptor expression profile of various human and animal tissues and cells. Serious confusion as to the structure of Butaprost was…
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BYL719
Cayman ChemicalA selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.
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Ciclesonide
Cayman ChemicalA corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.
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MMPIP (hydrochloride)
Cayman ChemicalA reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC50 = 26 nM).
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Oleyloxyethyl Phosphorylcholine
Cayman ChemicalOleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC50 value of 6.2 µM for porcine pancreatic PLA2.
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IWP-2-V2
Cayman ChemicalA less potent IWP-2 derivative that has been used to determine which structural features of IWP-2 are essential for impairing Wnt/ β-catenin pathway activity.
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Apelin-13
Cayman ChemicalEndogenous ligand of the APJ receptor, with an EC50 of 0.37 nM; acts primarily in the periphery and CNS, playing important roles in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.
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(±)-Nutlin-3
Cayman ChemicalAn inhibitor of p53-Mdm2 interaction (IC50 = 0.09 µM); induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53.
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3-bromo-5-phenyl Salicylic Acid
Cayman ChemicalSelective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC50 = 460 nM).
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N-acetyl-S-farnesyl-L-Cysteine
Cayman ChemicalAFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.
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Sphingosine-1-Phosphate
Cayman ChemicalA potent lipid signaling molecule that exhibits a wide range of biological activities; it enhances cell growth and inhibits the normal apoptotic response to a variety of stimuli.
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DAN-1 EE (hydrochloride)
Cayman ChemicalDAN-1 EE is a fluorescent indicator for the bioimaging of NO. DAN-1 EE is a cell permeable derivative of DAN, a molecule which has been used extensively in the quantitation of nitrate and nitrite using fluorescence spectroscopy. Upon entry into the cell, DAN-1 EE is transformed into the less cell…
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K252c
Cayman ChemicalK252c is a cell-permeable PKC inhibitor (IC50s = 2.45 and 25.7 µM for PKC and PKA, respectively). It induces apoptosis in human chronic myelogenous leukemia cancer cells. In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains…
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SIRT1/2 Inhibitor IV
Cayman ChemicalA cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM); less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a…
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EPZ015666
Cayman ChemicalA potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.
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ISCK03
Cayman ChemicalA cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.
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Pirlimycin
Cayman ChemicalA lincosamide antibiotic effective against Gram-positive bacteria that acts by inhibiting bacterial protein synthesis via binding to the 50S subunit of the ribosome.
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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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Hexanolamino PAF C-16
Cayman ChemicalHexanolamino PAF C-16 is a PAF analog with mixed PAF receptor agonist/antagonist properties. In human monocyte-derived macrophages, it is an antagonist which inhibits the production of reactive oxygen species in response to PAF C-16. On the other hand, in rabbit platelets and guinea pig…
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CAY10678
Cayman ChemicalA benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…
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TC 14012
Cayman ChemicalAn antagonist of CXCR4, blocking CXCR4-mediated HIV infection with an IC50 value of 19.3 nM; at 100 μg/ml, inhibits CXCL12-induced phosphorylation of p42/44 MAPK and STAT3; activates CXCR7 (EC50 = 350 nM), resulting in the recruitment of β-arrestin and Erk ½ phosphorylation.
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StemRegenin 1 (hydrochloride)
Cayman ChemicalA purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC50 = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC50 = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…
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ML-277
Cayman ChemicalA potent activator of KCNQ1 (Kv7.1) channels (EC50 = 260 nM); EC50 > 30 µM for KCNQ2, KCNQ4, and hERG; potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments IKs current in cultured…
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Chymostatin
Cayman ChemicalA potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.
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13-OAHSA
Cayman ChemicalA form of FAHFA in which oleic acid is esterified to 13-hydroxy stearic acid.
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IWP-3
Cayman ChemicalAn inhibitor of Wnt production that impairs Wnt pathway activity (IC50 = 40 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; promotes stem cell differentiation.