2,4-Difluoro-3-(methoxymethyl)benzoic+acid
Supplier:
Adipogen
Description:
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. AMG-47 is one of two optimized chemical compounds that has been shown to be extremely effective in vivo and in vitro in inhibiting Lck as well as a number of other receptor tyrosine kinases. In an anti-CD3/ IL-2 mouse model system AMG-47 has been shown to be effective in inhibiting the Lck mediated anti-inflammatory activity (ED50 11 mg/kg; 630nM) in vivo. In multiple other in vitro assays, AMG-47 exhibits subnanomolar inhibition against Lck, and low (<lt/>10nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK alpha (p38alpha). Moreover at slightly higher doses but well under 10µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2µM.
Catalog Number:
(76010-224)
Supplier:
Prosci
Description:
N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate-gated ion channels. These receptors have been shown to be involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. NMDA receptor channels are heteromers composed of the key receptor subunit NMDAR1 (GRIN1) and 1 or more of the 4 NMDAR2 subunits: NMDAR2A (GRIN2A), NMDAR2B (GRIN2B), NMDAR2C (GRIN2C) and NMDAR2D (GRIN2D). Alternatively spliced transcript variants encoding different isoforms have been found for this gene.
Catalog Number:
(75933-686)
Supplier:
Rockland Immunochemical
Description:
The ZBTB family of proteins is comprised of diverse zinc finger proteins that also contain a BTB (BR-C, ttk and bab) domain. While little is known about ZBTB40, other ZBTB proteins, such as ZBTB4 bind methylated DNA and repress transcription. Single nucleotide polymorphisms near ZBTB40 have been linked to differences in bone mineral density of the hip and lumbar spine, and had a significant association with low-trauma fractures suggesting that ZBTB40 may be involved in bone development and formation.
Catalog Number:
(76010-970)
Supplier:
Prosci
Description:
The protein encoded by this gene is a bifunctional enzyme that is involved in the peroxisomal beta-oxidation pathway for fatty acids. It also acts as a catalyst for the formation of 3-ketoacyl-CoA intermediates from both straight-chain and 2-methyl-branched-chain fatty acids. Defects in this gene that affect the peroxisomal fatty acid beta-oxidation activity are a cause of D-bifunctional protein deficiency (DBPD). An apparent pseudogene of this gene is present on chromosome 8. [provided by RefSeq].
Catalog Number:
(76010-136)
Supplier:
Prosci
Description:
ETFA participates in catalyzing the initial step of the mitochondrial fatty acid beta-oxidation. It shuttles electrons between primary flavoprotein dehydrogenases and the membrane-bound electron transfer flavoprotein ubiquinone oxidoreductase. Defects in electron-transfer-flavoprotein have been implicated in type II glutaricaciduria in which multiple acyl-CoA dehydrogenase deficiencies result in large excretion of glutaric, lactic, ethylmalonic, butyric, isobutyric, 2-methyl-butyric, and isovaleric acids. Two transcript variants encoding different isoforms have been found for this gene.
Catalog Number:
(10751-260)
Supplier:
Prosci
Description:
MYOZAP Antibody: MYOZAP, also known as GRINL1A, is a 54 kDa highly conserved cardiac protein. It is strongly expressed in the heart and lung and is a novel component of intercalated disc. MYOZAP interacts with myosin phosphatase-RhoA interacting protein (MRIP) and acts as an activator of Rho-dependent SRF signaling. Knockdown study in zebrafish results in cardiomyopathy with severe dysfunction. The MYOZAP gene is part of a complex transcript unit that includes the gene for glutamate receptor, ionotropic, N-methyl D-aspartate-like 1A (GRINL1A). Transcription of this gene occurs at an upstream promoter, with two different groups of alternatively spliced variants: Gup for GRINL1A upstream transcripts and Gcom for GRINL1A combined transcripts.
Supplier:
Adipogen
Description:
Selumetinib (AZD6244) is a second-generation, orally available, potent and selective ATP non-competitive inhibitor of MEK 1/2. In direct assays, AZD6244 selectively inhibits purified active MEK1 and MEK2 with an IC(50) of 14nM, and AZD6244 has reported IC(50) values of <lt/>100nm for MEK1 in ELISA assays and in bindings assays against recombinant domains of MEK2, Kd values were 53nM for AZD6244. AZD6244 demonstrated very effective anti-proliferation effects against several different cell lines with IC(50) values ranging from a low of 3nM to <lt/> 1µM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC(50) concentrations <lt/> 40nM. AZD6244 has demonstrated potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin, and lung cancer, and inhibition of tumor growth was found to correlate with the reduction of phospho-ERK1/2 levels in tumors.
Catalog Number:
(10075-672)
Supplier:
Prosci
Description:
The ion channels activated by glutamate are typically divided into two classes. Those that are sensitive to N-methyl-D-aspartate (NMDA) are designated NMDA receptors (NMDAR). The NMDAR plays an essential role in memory, neuronal development and it has also been implicated in several disorders of the central nervous system including Alzheimer’s, epilepsy and ischemic neuronal cell death. Overexpression of the NR2B subunit of the receptor has been associated with increases in learning and memory while aged, memory impaired animals have deficiencies in NR2B expression. Tyr1472 on NR2B is phosphorylated and this may lead to the increased expression of the NMDAR at the synapse that plays a role in synaptic plasticity.
Catalog Number:
(10751-330)
Supplier:
Prosci
Description:
VASH1 Antibody: VASH1 was originally identified as an endothelium-derived vascular endothelial growth factor (VEGF)-inducible angiogenesis inhibitor that acts in a negative feedback manner. VASH1 mRNA is expressed brain, heart, kidney and placenta in the adult, with robust expression in various organs during embryonic development. VASH1 expression in tumor cells and tumor vasculature is silenced by methylation by increased expression of Zeste homolog 2 (EZH2). The increase of EZH2 expression is induced by VEGF stimulation, leading to poor clinical prognosis. Recombinant adenovirus expressing VASH prevented tumor angiogenesis and inhibited tumor growth, suggesting that it may be a potentially valuable antitumor therapy in the clinic.
Catalog Number:
(76011-368)
Supplier:
Prosci
Description:
Similar to acetylation and phosphorylation, histone methylation at the N-terminal tail has emerged as an important role in regulating chromatin dynamics and gene activity. Histone methylation occurs on arginine and lysine residues and is catalyzed by two families of proteins, the protein arginine methyltransferase family and the SET-domain-containing methyltransferase family. Five members have been identified in the arginine methyltransferase family. About 27 are grouped into the SET-domain family, and another 17 make up the PR domain family that is related to the SET domain family. The retinoblastoma protein-interacting zinc finger geneRIZ1 is a tumor suppressor gene and a FOUNDING member of the PR domain family. RIZ1 inactivation is commonly found in many types of human cancers and occurs through loss of mRNA expression, frame shift mutation, chromosomal deletion, and missense mutation. RIZ1 is also a tumor susceptibility gene in mice. The loss of RIZ1 mRNA in human cancers was shown to associate with DNA methylation of its promoter CpG island. Methylation of the RIZ1 promoter strongly correlated with lost or decreased RIZ1 mRNA expression in breast, liver, colon, and lung cancer cell lines as well as in liver cancer tissues.
Supplier:
Adipogen
Description:
Tozasertib, or VX-680, is a potent and selective inhibitor of Aurora kinases, particularly Aurora A and B. In vitro, VX-680 blocks cell cycle progression and induces apoptosis in a wide range of human tumor types at low IC(50) values (i.e. 3.38nM for human BE-13 cells, and 14.34nM for NTERA cells). Moreover, VX680, also has very potent Ki values, with inhibition constants (Ki) of 0.6, 18, and 46nM for Aurora A, B, and C, respectively. VX-680 is also effective in vivo, being used in a Caki-1 xenograft model, VX-680 demonstrated a 75.7% (P < 0.001) decrease in Caki-1 xeno-graft tumor volume with no apparent alternation in animal body weight, peripheral blood counts, or other biological parameters.
Catalog Number:
(76008-842)
Supplier:
Prosci
Description:
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, 3 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 ES cells but their expression is down regulated in differentiating ES cells and is low in adult somatic tissue. Dnmt1 co-purifies with the retinoblastoma (Rb) tumour suppressor gene product, E2F1, and HDAC1. Dnmt1 also cooperates with Rb to repress transcription from promoters containing E2Fbinding sites suggesting a link between DNA methylation, histone deacetylase and sequence-specific DNA binding activity, as well as a growth-regulatory pathway that is disrupted in nearly all cancer cells.
Catalog Number:
(10082-134)
Supplier:
Proteintech
Description:
Four-and-a-half LIM domains 1 (FHL1), a member of the FHL protein family, which composed of FHL 1, 2, 3, 4 and ACT (activator of CREM), and characterized by an N-terminal half LIM domain followed by four complete LIM domains. FHL1 may contribute to sarcomere synthesis, assembly and biomechanical stress sensing. FHL1 is also a methylation-silenced tumor-suppressor gene on chromosome X in gastrointestinal cancers, which contributes to the formation of an epigenetic field for cancerization. FHL1(10991-1-AP) is highly expressed in skeletal muscle and to a lesser extent in heart, placenta, ovary, prostate, testis, small intestine, colon and spleen. This is a rabbit polyantibody raised against full length of human FHL1.
Catalog Number:
(89416-004)
Supplier:
Prosci
Description:
LSD1 Antibody: Histone modifications mediate changes in gene expression by altering chromatin structure or by serving as a platform to recruit other proteins. LSD1 is a recently discovered amine oxidase that catalyzes the lysine-specific demethylation of histone proteins via an FAD-dependent oxidative reaction. Methylation on histone H3-K9 is thought to play an important role in heterochromatin formation, while methylation on arginine and some lysine residues (such as H3-K4) is associated with active transcription. LSD1 associates with various proteins, including HDAC1/2, CoREST, and BHC80, that act to regulate LSD1 activity in vivo, and in a histone H3-K4-specific methylase complex that is involved in transcriptional regulation. Experiments have shown that CoREST, a SANT domain-containing corepressor acts to enhance LSD1 activity, while BHC80, a PHD domain-containing protein, inhibits CoREST/LSD1 activity in vitro. LSD1-mediated histone demethylation thus may have significant effects on gene expression.
Catalog Number:
(10748-556)
Supplier:
Prosci
Description:
LSD1 Antibody: Histone modifications mediate changes in gene expression by altering chromatin structure or by serving as a platform to recruit other proteins. LSD1 is a recently discovered amine oxidase that catalyzes the lysine-specific demethylation of histone proteins via an FAD-dependent oxidative reaction. Methylation on histone H3-K9 is thought to play an important role in heterochromatin formation, while methylation on arginine and some lysine residues (such as H3-K4) is associated with active transcription. LSD1 associates with various proteins, including HDAC1/2, CoREST, and BHC80, that act to regulate LSD1 activity in vivo, and in a histone H3-K4-specific methylase complex that is involved in transcriptional regulation. Experiments have shown that CoREST, a SANT domain-containing corepressor acts to enhance LSD1 activity, while BHC80, a PHD domain-containing protein, inhibits CoREST/LSD1 activity in vitro. LSD1-mediated histone demethylation thus may have significant effects on gene expression.
Catalog Number:
(103007-966)
Supplier:
Anaspec Inc
Description:
This peptide is a histone H3 trimethylated at lysine 4 and is associated with transcription, specifically marking the transcription start site of actively transcribed genes. This peptide can be demethylated by Jumonji AT-rich interactive domanin 1 (JARID1) or by lysine demethylase 5 (KDM5) family of lysine demethylases.
Sequence: ART-K(Me3)-QTARKSTGGKAPRKQLA MW: 2296.6 Da % peak area by HPLC: 95 Storage condition: -20 °C
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