Cayman Chemical New Products

07-02 · 17(S)-HpDoHE

17(S)-HpDoHE is a mono-oxygenation product of docosahexaenoic acid in human whole blood, human leukocytes, human glial cells, and murine brain.17(S)-HpDoHE is generally reduced to 17(S)-HDoHE (Catalog No.10009799), a compound that serves as a precursor to 17(S)-resolvins.17(S)-HDoHE has been shown to inhibit TNF-α-induced interleukin-1β expression in human glioma cells and inhibit TNF-α-induced leukocyte trafficking to the murine air pouch.

07-02 · CAY10587

The free fatty acid receptor 1 (FFA1/GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids. There is evidence of a link between FFA1/GPR40 and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders. CAY10587 is a selective FFA1/GPR40 agonist (EC50 = 32 nM) that does not exhibit activity on the related FFA receptors FFA2/GPR43 or FFA3/GPR41. At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.

07-01 · 4-Methylbenzamide oxime

4-Methylbenzamide oxime is intended to be used as a building block in drug discovery chemistry.

07-01 · DNA Methyltransferase 3a Monoclonal Antibody (Clone 64B814.1)

Methylation of DNA at cytosine residues plays an important role in regulation of gene expression, genomic imprinting, and is essential for mammalian development. Hypermethylation of CpG islands in tumor suppressor genes or hypomethylation of bulk genomic DNA may be linked with development of cancer. To date, three families of mammalian DNA methyltransferase genes have been identified which include DNMT1, DNMT2, and DNMT3. DNMT1 is constitutively expressed in proliferating cells and inactivation of this gene causes global demethylation of genomic DNA and embryonic lethality. DNMT2 is expressed at low levels in adult tissues and its inactivation does not affect DNA methylation or maintenance of methylation. The DNMT3 family members, DNMT3a and DNMT3b, are strongly expressed in embryonic stem (ES) cells but their expression is down regulated in differentiating ES cells and is low in adult somatic tissue. Recently, it has been shown that naturally occurring mutations of DNMT3b gene occurs in patients with a rare autosomal recessive disorder, termed ICF (immunodeficiency, centromeric instability, and facial anomalies) syndrome.

06-30 · CB13

CB13 is a dual agonist of the CB1 (IC50 = 15 nM) and CB2 (IC50 = 98 nM) receptors. In rats, oral CB13 (3 mg/kg) potently blocks CB1-dependent neuropathic mechanical hyperalgesia, shows limited brain penetration, and exhibits good oral bioavailability. CB13 does not possess genotoxic potential, as indicated by negative results in both chromosome aberration and reverse mutation assays. The effects of CB13 on other aspects of CB signaling have not been assessed.

06-30 · FKGK 11

Phospholipase A2 catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. The three broad classes of phospholipase A2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%. In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.

06-30 · Hydroxyalprazolam-d5

Alprazolam is a triazolobenzodiazepine compound with anti-anxiety and sedative-hypnotic actions, that is eficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorder.

06-30 · β-Amyloid (1-8) Peptide

β-Amyloid peptide (1-42) aggregation results in the formation of neurotoxic fibrils or globular oligomers. This peptide is the control compound for tests that use Cayman’s β-Amyloid (1-8, A2V) Peptide (Catalog No. 10229). The use of these peptides along with β-amyloid (1-40 or 1-42) peptides may provide guidance in developing β-amyloid peptide aggregation inhibitors.

06-29 · N-3-oxo-octanoyl-L-Homoserine lactone

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases. AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family. In the gram-negative bacterium A. tumefaciens, N-3-oxo-octanoyl-L-homoserine lactone (3-oxo-C8-HSL) promotes the expression of the transcriptional activator (and LuxR homolog) TraR.

06-29 · PtdIns-(1-arachidonoyl)-d8)-(2-arachidonoyl) (sodium salt)

PtdIns-(1-arachidonoyl)-d8)-(2-arachidonoyl) (sodium salt) contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions. It is intended for use as an internal standard for the quantification of PtdIns-(1-arachidonoyl)-(2-arachidonoyl) (sodium salt) by GC- or LC-MS. The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals.

06-25 · Amiodarone-d4 (hydrochloride)

Aminodarone is an anti-anginal and anti-arrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting Na, potassium-activated myocardial adenosine triphosphatase. There is a resulting decrease in heart rate and in vascular resistance.

06-25 · (R)-(+)-Acenocoumarol

Acenocoumarol is a short-lived oral anti-coagulant, which, like warfarin, functions by inhibiting vitamin K epoxide reductase. It has higher intrinsic anticoagulant potency than warfarin and phenprocoumon, when evaluated in vitro. Acenocoumarol has a single chiral center that gives rise to two different enantiomeric forms. (R)-(+)-Acenocoumarol has a longer plasma elimination half-life (6.6 hours) and slower plasma clearance (1.9 L/h), compared to the (S)-(-)-enantiomer (1.8 hours, 28.5 L/h). The R-enantiomer is rapidly absorbed from the gastrointestinal tract with essentially complete oral bioavailability, whereas (S)-(-)-acenocoumarol undergoes extensive first-pass metabolism. Perhaps related to these pharmacokinetic characteristics, (R)-(+)-acenocoumarol is more potent in vivo as an anti-coagulant than the (S)-(-)-enantiomer. As the clearance of acenocoumarol is ~20-fold faster than that for warfarin, the plasma concentrations of acenocoumarol are substantially lower than those for warfarin in patients receiving long-term treatment.

06-25 · (S)-(-)-Acenocoumarol

Acenocoumarol is a short-lived oral anti-coagulant, which, like warfarin, functions by inhibiting vitamin K epoxide reductase. It has higher intrinsic anticoagulant potency than warfarin and phenprocoumon, when evaluated in vitro. Acenocoumarol has a single chiral center that gives rise to two different enantiomeric forms. (S)-(-)-Acenocoumarol has a shorter plasma elimination half-life (1.8 hours) and faster plasma clearance (28.5 L/h), compared to the (R)-(+)-enantiomer (6.6 hours, 1.9 L/h). The S-enantiomer undergoes extensive first-pass metabolism during absorption from the gastrointestinal tract, whereas (R)-(+)-acenocoumarol is rapidly absorbed and provides essentially complete oral bioavailability. Perhaps related to these pharmacokinetic characteristics, (S)-(-)-acenocoumarol is less potent in vivo as an anti-coagulant than the (R)-(+)-enantiomer. As the clearance of acenocoumarol is ~20-fold faster than that for warfarin, the plasma concentrations of acenocoumarol are substantially lower than those for warfarin in patients receiving long-term treatment.

06-25 · Thiamet G

Hyperphosphorylation of the tau protein leads to its aggregation and formation of neurofibrillary tangles, a hallmark of Alzheimer’s disease and other tauopathic, neurodegenerative disorders. Tau is also dynamically modified by the addition and cleavage of O-linked β-N-acetylglucosamine (O-GlcNAc) moieties, which is mediated in part by O-GlcNAcase. Levels of O-GlcNAcylated proteins from Alzheimer’s disease brain extracts are decreased as compared to that in controls, suggesting that impaired brain glucose metabolism may contribute to pathogenesis. Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM. It increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day). Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.

06-24 · CBHA

Histone deacetylase (HDAC) inhibitors hyperacetylate histones and increase transcriptional activity in selected genes. Importantly, HDAC inhibitors induce apoptosis in some cancer cells and show promise in the treatment of certain forms of cancer. CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 0.01 and 0.07 μM in vitro for HDAC1 and HDAC3, respectively. CBHA also induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM) and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg. The efficacy of CBHA for suppressing tumor growth in mice is enhanced by the addition of retinoic acid.

06-23 · CAY10589

Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM). It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.

06-23 · CAY10594

Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles.CAY10594 is a potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM). It is also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells). CAY10594 strongly inhibits the invasive migration of breast cancer cells in transwell assays, suggesting that PLD might be a useful target in blocking tumor cell invasion.

06-23 · Goat Anti-Mouse: SureLight® P-3L

Spectral Characteristics: Visible absorption maxima=614>650 (sh) nm, Emission maximum=662 nm; This goat anti-mouse P-3L is used as the 'secondary antibody' for immunofluorescent staining on tissues or culture cells where the primary antibody is generated in mice. It is highly recommended that proper negative controls, such as omitting the primary antibody, be included in experiments when conducting immunofluorescent staining.

06-18 · Avenanthramide-C methyl ester

Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM). Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells.

06-18 · CAY10603

Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively). Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM). The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroamic acid (SAHA).