Biologically Active Small Molecules, 1 mg, Cayman Chemical
-
CX-5461
Cayman ChemicalA selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC50s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.
-
Eggmanone
Cayman ChemicalA selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation.
-
-
11-keto-ß-Boswellic Acid
Cayman Chemical11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). Boswellic acids are specific, non-redox inhibitors of leukotriene synthesis via 5-lipoxygenase that demonstrate anti-inflammatory…
-
(S)-p38 MAP Kinase Inhibitor III
Cayman ChemicalA methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 µM in vitro); potently blocks the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 µM, respectively).
-
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,…
-
T-2 Toxin
Cayman ChemicalA trichothecene mycotoxin that can infect grain crops causing alimentary toxic aleukia in humans and animals; inhibits protein synthesis, disrupts membrane phospholipid metabolism, increases lipid peroxides in the liver, and is highly cytotoxic to macrophages (IC50 = 19.47 nM), altering the…
-
Ac-YVAD-pNA
Cayman ChemicalA colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.
-
-
RAD140
Cayman ChemicalAD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM. At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats. At…
-
Ponasterone A
Cayman ChemicalAn insect hormone used as an inducer of ecdysone-inducible mammalian expression systems.
-
MRS1523
Cayman ChemicalA selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).
-
Verteporfin
Cayman ChemicalA photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration; also inhibits autophagosome formation by directly targeting and modifying p62, a scaffold and adaptor protein that binds both…
-
Resminostat (hydrochloride)
Cayman ChemicalAn orally bioavailable inhibitor of HDAC1, HDAC3, and HDAC6 (IC50s = 43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells; abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC50s = 2.5-3 µM); dose-dependently…
-
-
a-Amanitin
Cayman ChemicalA mycotoxin that selectively inhibits RNA polymerase II (1 µg/ml), preventing translocation of the enzymes on DNA; used in molecular biology to distinguish among types of RNA polymerase in a sample and to arrest RNA synthesis in transcription studies.
-
Ampkinone
Cayman ChemicalA small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…
-
CWHM12
Cayman ChemicalCWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC50s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…
-
Ingenol-3-angelate
Cayman ChemicalA hydrophobic diterpene ester that rapidly induces cell death in proliferating keratinocytes through plasma membrane and mitochondrial disruption; causes inflammation due, at least in part, to activation of PKC, leading to antibody-dependent cellular cytotoxicity.
-
N-(2-phenylethyl)-Indomethacin amide
Cayman ChemicalN-2PIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-2PIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.06 and 0.125 µM, respectively. It is over 400 times less potent as an inhibitor of…
-
17a,20ß-Dihydroxy-4-pregnen-3-one
Cayman ChemicalAn endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.
-
4-Methylumbelliferyl-ß-D-N,N',N''-Triacetylchitotrioside
Cayman ChemicalA fluorogenic substrate for chitinases and chitotriosidases.
-
KN-93 (hydrochloride)
Cayman ChemicalA selective inhibitor of CaMKII, competitively blocking CaM binding to the kinase (Ki = 370 nM); inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).
-
Sirtinol
Cayman ChemicalA cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.
-
Adenosine 5'-(?-thio)-triphosphate (lithium salt)
Cayman ChemicalA stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC50 = 5.52 for P2Y11).
-
5-Iodotubercidin
Cayman ChemicalInitiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).
-
Prostaglandin F1a
Cayman ChemicalPGF1α is the putative metabolite of DGLA via the COX pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10−11 M. PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the…
-
-
UNC1215
Cayman ChemicalA potent, selective chemical probe for the methyl lysine reading function of L3MBTL3 (Kd = 120 nM; IC50 = 40 nM) that competitively displaces mono- or dimethyl-lysine containing peptides.
-
SCR7 pyrazine
Cayman ChemicalA small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC50s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…
-
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…
-
Darglitazone
Cayman ChemicalA TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations; increases insulin effectiveness in obese NIDDM subjects; promotes adipocyte differentiation by up-regulating the expression of UCP-2.