Cayman Chemical New Products

03-16 · (+)-Abscisic Acid

Tue, 16 Mar 2010 00:00:00 EDT

Abscisic acid (ABA) is a plant hormone with diverse roles in disease resistance, plant development, and response to stresses (water, salt, temperature, and pathogens). It is also produced by some plant pathogenic fungi. In addition to key roles in regulating stomatal closing, seed dormancy, and cell division, ABA regulates gene expression and may contribute to epigenetic changes at the chromatin level. The (+)-enantiomer is the naturally occurring and more active form of ABA.

03-16 · HSP90α (human recombinant)

Tue, 16 Mar 2010 00:00:00 EDT

Heat shock proteins (Hsps) are molecular chaperones that can account for upwards of 1-2% of all cellular protein. The Hsp90 gene family consists of Hsp90A, Hsp90B, and TRAP subfamilies. The Hsp90A family is localized in the cytoplasm and can be further sub-divided into Hsp90AA (inducible) and Hsp90AB (constitutively expressed), yielding Hsp90α and Hsp90β proteins respectively. Hsp90B codes for the ER-localized protein Grp94, while TRAP, producing TRAP1, is a mitochondrial chaperone. Hsp90 acts as a dimer, which can be homo or heterodimers of the α and β isoforms, and functions to bind protein substrates that are unfolded and/or misfolded to assist in folding and prevent aggregation. C-terminus dimerization of Hsp90, coupled with the ATPase molecular clamp activity cause a conformational change in the N-terminal nucleotide binding domain thus facilitating substrate binding. Hsp90 associates with many co-chaperones including p23/Sba1, which help in recruiting substrates to the Hsp90 complex. Hsp90 works on many different substrates, however its activity seems to be more specific for protein kinases involved in signal transduction, steroid receptors, and cytoskeletal proteins.

03-16 · Hsp90β (human recombinant)

Tue, 16 Mar 2010 00:00:00 EDT

Heat shock proteins (Hsps) are molecular chaperones that can account for upwards of 1-2% of all cellular protein. The Hsp90 gene family consists of Hsp90A, Hsp90B, and TRAP subfamilies. The Hsp90A family is localized in the cytoplasm and can be further sub-divided into Hsp90AA (inducible) and Hsp90AB (constitutively expressed), yielding Hsp90α and Hsp90β proteins, respectively. Hsp90B codes for the ER localized protein Grp94, while TRAP, producing TRAP1, is a mitochondrial chaperone. Hsp90 forms either homo or heterodimers of the α and β isoforms which then bind protein substrates that are unfolded and/or misfolded to assist in folding and prevent aggregation. C-terminus dimerization of Hsp90, coupled with the ATPase molecular clamp activity, cause a conformational change in the N-terminal nucleotide binding domain thus facilitating substrate binding. Hsp90 associates with many co-chaperones, including p23/Sba1, which help in recruiting substrates to the Hsp90 complex. Hsp90 works on many different substrates, however its activity seems to be more specific for protein kinases involved in signal transduction, steroid receptors, and cytoskeletal proteins.

03-10 · AdPLA2 Polyclonal Antibody

Wed, 10 Mar 2010 00:00:00 EST

AdPLA2 is the first member of Group XVI phospholipase A2 (PLA2). The PLA2 superfamily consists of multiple enzymes that catalyze the hydrolysis of fatty acids from the sn-2 position in phospholipids. This pH- and calcium-dependent PL is highly expressed in adipose tissue and is associated with adipocyte differentiation and lipolysis. It has been implicated as a major player in the development of obesity. Human AdPLA2 is a 162 amino acid protein with a calculated molecular weight of 18 kDa. It contains a transmembrane region and shares 70-75% sequence similarity with the murine and rat proteins, respectively. Cayman’s antibody was raised against the C-terminal region of the human protein.

03-10 · PIK-75

Wed, 10 Mar 2010 00:00:00 EST

Phosphatidylinositol 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI3K family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation. In the class I PI3Ks, p110α is the primary PI3K isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors. Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM. It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively. In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.

03-10 · W146 (trifluoroacetate salt)

Wed, 10 Mar 2010 00:00:00 EST

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.

03-09 · SC-51322

Tue, 09 Mar 2010 00:00:00 EST

The prostaglandin E2 (PGE2) receptor (EP1) is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a murine writhing assay with an ED50 value of 0.9 mg/kg. It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089. SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.

03-09 · SET8 Methyltransferase Inhibitor Screening Assay Kit

Tue, 09 Mar 2010 00:00:00 EST

SET Domain-containing Protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20 (H4K20), an event proven to have an important role in chromatin structure and transcriptional activation. Cayman's SET8 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET8 inhibitors. The transfer of the methyl group from SAM by SET8 (provided in the kit) to the acceptor peptide (H4K20) generates S-adenosylhomocysteine, which is rapidly converted to urate and hydrogen peroxide (H2O2) using an enzyme mixture provided in the kit. The H2O2 formed is quantified using 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) to produce the highly fluorescent compound resorufin (excitation 530-540 nm; emission 585-595 nm).

03-09 · SureLight® Western Kit (P112)

Tue, 09 Mar 2010 00:00:00 EST

Save time and money with Columbia Bioscience's Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P112) features sensitive fluorescent detection with a Goat Anti-Mouse SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm^2 blots.

03-09 · SureLight® Western Kit (P114)

Tue, 09 Mar 2010 00:00:00 EST

Save time and money with Columbia Bioscience's Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P114) features sensitive fluorescent detection with a Goat Anti-Rabbit SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm^2 blots.

03-08 · 2-amino-4-phenyl Thiazole

Mon, 08 Mar 2010 00:00:00 EST

2-amino-4-phenyl Thiazole is a synthetic intermediate useful for pharmaceutical synthesis.

03-08 · Donepezil

Mon, 08 Mar 2010 00:00:00 EST

Acetylcholine is a neurotransmitter involved in neural signaling throughout the body. Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. It has a half-life in circulation of about 70 hours. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.

03-08 · Pristimerin

Mon, 08 Mar 2010 00:00:00 EST

Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-arachidonoyl glycerol (2-AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC50 = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 µM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).

03-08 · SET7/9 (FL) Polyclonal Antibody

Mon, 08 Mar 2010 00:00:00 EST

Diverse signal transduction pathways impinging on the N-terminal tails of histones lead to a number of post-translational modifications including acetylation, phosphorylation, poly (ADP-ribosylation), ubiquitination, and methylation. These modifications play critical roles in regulating chromatin structure and gene expression. Histone methyltransferases selectively methylate evolutionarily conserved arginine or lysine residues, primarily in the N-terminal tails of histones H3 and H4. SET7/9 utilizes S-adenosylmethionine to methylate histone H3 at lysine 4. Human SET7/9 is a 366 amino acid protein with observed migration on SDS-PAGE at 49 kDa.

03-04 · CYP3A4 Induction STEP™ Reporter Assay Kit (Luminescence)

Thu, 04 Mar 2010 00:00:00 EST

Early screening of a drug candidate's potential to induce or inhibit CYP3A4 is a critical step in the drug development process. Cayman's CYP3A4 Induction STEP™ Reporter Assay Kit (Luminescence) is a novel method to assess CYP3A4 induction. STEP™ (Surface Transfection and Expression Protocol) is a patented, solid phase transient transfection technology that overcomes many of the disadvantages of other transfection approaches. Cayman’s assay consists of a 96-well plate coated with a STEP™ complex containing a Secreted Alkaline Phosphatase (SEAP) reporter regulated by the human CYP3A4 gene promoter. The STEP™ complex also contains two nuclear expression constructs, Pregnane X Receptor (PXR) and Hepatocyte Nuclear Factor-4α (HNF-4α). Cells grown on the CYP3A4 STEP™ plate will introduce the reporter gene and express PXR and HNF-4α. Binding of inducer-activated transcription factors to the CYP3A4 promoter initiates expression of SEAP, which is secreted into the cell culture medium. Aliquots of medium are removed at fixed time intervals and SEAP activity is measured by adding a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is simple to use and can be easily adapted to high-throughput screening for potential CYP3A4 inducers.

03-04 · Palmitoyl Ethanolamide-d5

Thu, 04 Mar 2010 00:00:00 EST

Palmitoyl ethanolamide (PEA) is an endogenous cannabinoid found in brain, liver, and other mammalian tissues. PEA has also been isolated from egg yolk, and found to have anti-anaphylactic and anti-inflammatory activity in vitro. PEA is an endocannabinoid which has been shown to significantly elevate cAMP in cells expressing CB2 receptors. However, its affinity for CB2 receptors is relatively low, at about 10 µM. CB1 receptors have no appreciable affinity for PEA.

03-03 · CD36 Monoclonal Antibody (Clone JC63.1) (azide free)

Wed, 03 Mar 2010 00:00:00 EST

CD36 is a type-B scavenger receptor that is necessary for the formation of foam cells and thereby atherosclerotic lesions. This membrane glycoprotein can internalize fatty acids which activate PPARγ and stimulate further expression of CD36. This positive feedback loop combined with the murine CD36 knock-out studies reinforces the importance of CD36 in lipid metabolism. Additionally CD36 is needed for the phagocytosis of P. falciparum infected erythrocytes, retinal pigment epithelial cell photoreceptor fragments and post-apoptotic monocytes and neutrophils. CD36 expression has been monitored during hematopoietic cell differentiation and may be an indicator of tumor spreading in lymphocytic leukemia. Positive controls include adipose and heart tissue, platelets and macrophages.

03-01 · Corticosterone EIA Kit

Mon, 01 Mar 2010 00:00:00 EST

Corticosterone is a glucocorticoid produced by the adrenal cortex in response to ACTH (corticotropic hormone) and is the precursor to aldosterone. The production of glucorcorticoids is increased by stress; therefore, corticosterone can be used as a biomarker of stress. Biologists often measure corticosterone in fecal material of the species they are studying. This non-invasive sample collection procedure has the advantage of not itself causing stress and thereby increasing corticosterone levels, a common problem when samples for measurement of corticosterone are collected by more invasive means. Plasma corticosterone levels have a circadian variation and corticosterone may be important in the regulation of the sleep-wake cycle. The concentration of corticosterone in human plasma is approximately 0.9-3.9 ng/ml in females and 3.2-7.6 ng/ml in males. Cayman's Corticosterone EIA Kit is a competitive assay that can be used for quantification of corticosterone in plasma and fecal samples.

03-01 · HDAC4 (human recombinant)

Mon, 01 Mar 2010 00:00:00 EST

Histone deacetylases (HDACs) catalyze the deacetylation of core histones, resulting in tightening of nucleosomal integrity, restriction of the access of transcription factors, and suppression of transcription. HDACs also play important roles in mediating nuclear receptor functions by forming co-repressor complexes with nuclear receptors in the absence of ligands. They are also involved in mediating other transcription regulatory pathways by associating with transcription factors, such as E2F, TFIIE, TFIIF, NF-kB, p300, Stat3, p53, and the retinoblastoma (Rb) protein. HDAC4 is a Class IIa HDAC which is homologous to yeast Hda 1 and is larger in size than the other 2 classes of HDACs. Class IIa HDACs contain a highly conserved C-terminal deacetylase catalytic domain (~420 amino acids) and an N-terminal domain with no similarity to HDACs in other classes. Class II HDACs can shuttle between the nucleus and cytoplasm, suggesting potential extranuclear functions by regulating the acetylation status of nonhistone substrates. By modifying chromatin structure and other nonhistone proteins, HDACs play important roles in controlling complex biological events, including cell development, differentiation, programmed cell death, angiogenesis, and inflammation. Considering these major roles, it is conceivable that dysregulation of HDACs and subsequent imbalance of acetylation and deacetylation may be involved in the pathogenesis of various diseases, including cancer and inflammatory diseases.

02-25 · H-1152 (hydrochloride)

Thu, 25 Feb 2010 00:00:00 EST

Rho kinase (ROCK), activated by GTP-linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM). H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension.