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131533 results for "CAFRAMO+LTD+CA&pageNo=10"

131533 Results for: "CAFRAMO+LTD+CA&pageNo=10"

Human Recombinant HGF (from (BTI-Tn-5B1-4) Hi-5 Insect cells)

Supplier: Peprotech

HGF is a potent, mesenchymally-derived mitogen for mature parenchymal hepatocytes, and acts as a growth factor for a broad spectrum of tissues and cell types. HGF signals through a transmembrane tyrosine kinase receptor known as MET. Activities of HGF include the induction of cell proliferation, motility, morphogenesis, inhibition of cell growth, and enhancement of neuron survival. HGF is a crucial mitogen for liver regeneration processes, especially after partial hepatectomy and other liver injuries. Human and murine HGF are cross-reactive. Human HGF is expressed as a linear, polypeptide-precursor glycoprotein containing 697 amino acid residues. Proteolytic processing of this precursor generates the biologically active heterodimeric form of HGF, which consists of two polypeptide chains (α-chain and β-chain) held together by a single disulfide bond resulting in formation of a biologically active heterodimer. The α-chain consists of 463 amino acid residues and four kringle domains. The β-chain consists of 234 amino acid residues. Recombinant Human HGF is an 80.0 kDa polypeptide consisting of 697 amino acid residues.

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Human Recombinant PDGF-BB (from E. coli)

Supplier: Peprotech

PDGFs are disulfide-linked dimers consisting of two 12.0-13.5 kDa polypeptide chains, designated PDGF-A and PDGF-B chains. The three naturally occurring PDGFs, PDGF-AA, PDGF-BB and PDGF-AB, are potent mitogens for a variety of cell types, including smooth muscle cells, connective tissue cells, bone and cartilage cells, and some blood cells. The PDGFs are stored in platelet α-granules, and are released upon platelet activation. The PDGFs are involved in a number of biological processes, including hyperplasia, chemotaxis, embryonic neuron development, and respiratory tubule epithelial cell development. Two distinct signaling receptors used by PDGFs have been identified and named PDGFR-α and PDGFR-β. PDGFR-α is a high-affinity receptor for each of the three PDGF forms. On the other hand, PDGFR-β interacts with only PDGF-BB and PDGF-AB. Recombinant Human PDGF-BB is a 24.3 kDa disulfide-linked homodimer of two β chains (218 total amino acids).

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Human Recombinant TNF-alpha (from E. coli)

Supplier: Peprotech

TNF-α is a pleiotropic pro-inflammatory cytokine secreted by various cells, including adipocytes, activated monocytes, macrophages, B cells, T cells and fibroblasts. It belongs to the TNF family of ligands, and signals through two receptors, TNFR1 and TNFR2. TNF-α is cytotoxic to a wide variety of tumor cells, and is an essential factor in mediating the immune response against bacterial infections. TNF-α also plays a role in the induction of septic shock, autoimmune diseases, rheumatoid arthritis, inflammation, and diabetes. Human and murine TNF-α demonstrate significant cross-species reactivity. TNF-α exists in two forms; a type II transmembrane protein, and a mature soluble protein. The TNF-α transmembrane protein is proteolytically cleaved to yield a soluble, biologically active, 17 kDa TNF-α, which forms a non-covalently linked homotrimer in solution. Recombinant Human TNF-α is a soluble 157 amino acid protein (17.4 kDa) which corresponds to C-terminal extracellular domain of the full length transmembrane protein.

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Human Recombinant Heregulin Beta1 (from E. coli)

Supplier: Peprotech

Neuregulin/Heregulin is a family of structurally related polypeptide growth factors derived from alternatively spliced genes (NRG1, NRG2, NRG3 and NRG4). To date, there are over 14 soluble and transmembrane proteins derived from the NRG1 gene. Proteolytic processing of the extracellular domain of the transmembrane NRG1 isoforms releases soluble growth factors. HRG1-β1 contains an Ig domain and an EGF-like domain; the latter is necessary for direct binding to receptor tyrosine kinases erb3 and erb4. This binding induces erb3 and erb4 heterodimerization with erb2, stimulating intrinsic kinase activity that leads to tyrosine phosphorylation. Although HRG1-β1's biological effects are still unclear, it has been found to promote motility and invasiveness of breast cancer cells, which may also involve up-regulation of expression and function of the autocrine motility-promoting factor (AMF). Recombinant Human Heregulinβ-1 (HRG1-B1) is a 7.5 kDa polypeptide consisting of only the EGF domain of heregulinβ-1 (65 amino acid residues). Manufactured using all Animal-Free reagents.

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RPLCMNT MTR CTRL 78018 MINIFLX

Supplier: Avantor Fluid Handling

RPLCMNT MTR CTRL 78018 MINIFLX

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β-(N-Morpholino)ethanesufonic acid (MES) monohydrate ≥99%, white crystalline powder for molecular biology

Supplier: MP Biomedicals

MES is a zwitterionic buffer. One of the "Good" buffers developed for biological applications. It has the advantages of maximum water solubility and minimum solubility in all other solvents, minimal salt effects, minimal change in pK with temperature, chemically and enzymatically stable, minimal absorption in visible or UV spectral range.
A buffer using MES free acid can be prepared by titrating the free acid with sodium hydroxide to the desired pH (pKa ± 1). Alternatively, volumes of equimolar MES free acid and sodium or potassium MES can be mixed to attain the desired pH.

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Glutaraldehyde solution 50% in aqueous solution

Supplier: MP Biomedicals

Glutaraldehyde is a bifunctional protein cross-linking reagent, reacting with NH2 groups to form Schiff's bases.
Sporicidal agent. Glutaraldehyde reacts through cross-linking to impart water resistance to protein and polyhydroxy compounds. It is also a reducing agent for photochemicals. In organic syntheses, the reactive carbonyl groups of glutaraldehyde suggest its use as an intermediate for the production of resins, dyestuffs, and pharmaceuticals. Glutaraldehyde is a disinfectant, which is rapidly effective against vegetative forms of Gram-positive and Gram-negative bacteria. It is also effective against acid-fast bacteria, bacterial spores, some fungi and viruses, including hepatitis B virus and human immunodeficiency virus. It can also be used for stabilization of proteins on agarose beads, activation of polystyrene and glass for immobilization of antibodies and antigens, and coupling peptides onto carrier proteins. Can be used for preparing emulsions for making photographic film. Also for use as an electron microscopy fixative or cell fixation.
Store at +4 °C. Store Under Nitrogen

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Anti-FOXJ1 Rabbit Polyclonal Antibody

Anti-FOXJ1 Rabbit Polyclonal Antibody

Supplier: Prosci

FOXJ1 is a member of forkhead/winged-helix transcription factor family, which play crucial roles during vertebrate development. FOXJ1 may play an important role in cell fate determination during lung development and in spermatogenesis.The unique pattern of FOXJ1expression during human fetal development suggests a role for this forkhead/winged-helix factor during pulmonary and renal epithelial development. Single nucleotide polymorphisms were identified in FOXJ1 and a significant association was found with allergic rhinitis.FOXJ1 is a member of the forkhead gene family, which was originally identified in Drosophila. The forkhead family is composed of transcription factors with a conserved 100-amino acid DNA-binding motif.FOXJ1 is a member of the forkhead gene family, which was originally identified in Drosophila. The forkhead family is composed of transcription factors with a conserved 100-amino acid DNA-binding motif.

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Anti-CD27 Mouse Monoclonal Antibody (APC (Allophycocyanin)) [clone: O323]

Anti-CD27 Mouse Monoclonal Antibody (APC (Allophycocyanin)) [clone: O323]

Supplier: Tonbo Biosciences

The O323 antibody reacts with human CD27 (TNFRSF7), a cell surface homodimer of 55 kDa subunits, which provides co-stimulatory signaling in support of the T cell (TCR) and B cell (BCR) receptors. By comparison with CD28, whose TCR co-stimulatory signal can trigger cell proliferation, CD27 signaling appears to promote cell survival and differentiation to effector / memory stages. Also in contrast with CD28, the CD27 receptor may be shed following interaction with its ligand CD70, which is typically expressed on activated dendritic cells, T cells and B cells. With respect to B cells, CD27 is considered to be a phenotypic marker for memory B cells. CD27 has been included within a group of phenotypic markers for identifying human B regulatory cells (Bregs), a cell type proposed to regulate CD4+ T cell proliferation and Foxp3 / CTLA-4 expression in Treg cells.

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Anti-EPHB2 Rabbit Polyclonal Antibody

Anti-EPHB2 Rabbit Polyclonal Antibody

Supplier: Prosci

EphrinB proteins are thought to play key roles in cellular functions as diverse as neuronal migration and blood vessel development (Flanagan and Vancerhaeghen, 1998; Dufour et al., 2003; Oike et al., 2002). EphrinB molecules expressed at the membrane surface bind to the EphB family receptors on target cells during cellto cell contact. This interaction leads to cell signaling in the target cell but also generates a reverse signal in the cell expressing EphrinB on its surface. This reverse signaling event is thought to be critical for vessel maturation and neuronal development. Importantly, tyrosine phosphorylation of EphrinB is thought to be a critical component of this reverse signaling event (Palmer et al., 2002). Recent work suggests that phosphorylation of a specific EphrinB residue (Tyr298) plays a key role in EphrinB signaling (Kalo, et al., 2001).

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Anti-TPH2 Rabbit Polyclonal Antibody

Anti-TPH2 Rabbit Polyclonal Antibody

Supplier: Prosci

Tryptophan hydroxylase (TPH) catalyzes the 5-hydroxylation of tryptophan, which is the first step in the biosynthesis of indoleamines (serotonin and melatonin) (Martinez et al., 2001). In mammals, serotonin biosynthesis occurs predominantly in neurons which originate in the Raphe nuclei of the brain, and melatonin synthesis takes place within the pineal gland. Although TPH catalyzes the same reaction within the Raphe nuclei and the pineal gland, TPH activity is rate-limiting for serotonin but not melatonin biosynthesis. Serotonin functions mainly as a neurotransmitter, whereas melatonin is the principal hormone secreted by the pineal gland. The activity of TPH is enhanced by phosphorylation by cAMP-dependent protein kinase (PKA) and Ca2+/calmodulin kinase II (CaM K II) (Jiang et al., 2000; Johansen et al., 1996). CaM K II phosphorylates Ser19 which lies within the regulatory domain of TPH2 (McKinney et

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Anti-ALKBH2 Rabbit Polyclonal Antibody

Anti-ALKBH2 Rabbit Polyclonal Antibody

Supplier: Rockland Immunochemical

The E. coli AlkB protein protects against the cytotoxicity of methylating agents by repair of the specific DNA lesions generated in single-stranded DNA; ALKBH2 and ALKBH3 are mammalian homologs of AlkB that catalyze the removal of 1-methyladenine and 3-methylcytosine, modifications that left unchecked could lead to cancerous cells. Mutations in both ALKBH2 and ALKBH3 have been observed in pediatric brain tumors indicating that these proteins are important in the prevention of cancer formation. Like the histone demethylase JMJD1A, ALKBH2 is a non-heme iron enzyme that is inhibited by Nickel ions, suggesting that inhibition of ALKBH2 by Nickel ions may play a role in the development of cancer. Conversely, ALKBH2 mRNA and protein levels are increased glioma cells following Photofrin-mediated photodynamic therapy, an adjuvant therapy in cancer treatment, suggesting that down-regulating ALKBH2 expression in cancer cells may enhance the anti-cancer effectiveness of this treatment.

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Bovine Fibrinogen (from Plasma), MP Biomedicals

Bovine Fibrinogen (from Plasma), MP Biomedicals

Supplier: MP Biomedicals

Background Information
Fibrinogen is a blood protein that is involved in clotting and is converted to fibrin by thrombin. Fibrinogen has an approximate molecular weight of 340 kDa. It consists of three non-identical pairs of disulfidebonded chains. The α-chain has an approximate molecular weight of 63.5 kDa, the β-chain 56 kDa, and the γ-chain 47 kDa. At the amino termini, the three chains are connected in a dimeric disulfide knot (DSK). A second DSK occurs later in the molecule. Fibrinogen has approximately 4% carbohydrate content.

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Anti-CD120b (TNF R Type II/p75) Armenian Hamster Monoclonal Antibody (Biotin) [clone: TR75-32.4]

Supplier: Biolegend

Biotin anti-mouse CD120b (TNF R Type II/p75) [TR75-32.4]; Isotype: Armenian Hamster IgG; Reactivity: Mouse; Apps: FC, ELISA Detection; Size: 50 μg

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Mouse Recombinant PDGF-BB (from E. coli)

Supplier: Peprotech

PDGFs are disulfide-linked dimers consisting of two 12.0-13.5 kDa polypeptide chains, designated PDGF-A and PDGF-B chains. The three naturally occurring PDGFs, PDGF-AA, PDGF-BB and PDGF-AB, are potent mitogens for a variety of cell types, including smooth muscle cells, connective tissue cells, bone and cartilage cells, and some blood cells. The PDGFs are stored in platelet α-granules, and are released upon platelet activation. The PDGFs are involved in a number of biological processes, including hyperplasia, chemotaxis, embryonic neuron development, and respiratory tubule epithelial cell development. Two distinct signaling receptors used by PDGFs have been identified and named PDGFR-α and PDGFR-β. PDGFR-α is a high-affinity receptor for each of the three PDGF forms. On the other hand, PDGFR-β interacts with only PDGF-BB and PDGF-AB. Recombinant Murine PDGF-BB is a 24.4 kDa disulfide-linked homodimer of two β chains (218 total amino acids).

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Anti-CD34 Mouse Monoclonal Antibody [clone: SPM610]

Supplier: Prosci

This antibody recognizes a carbohydrate epitope on a single chain, transmembrane, heavily glycosylated protein of 90-120kDa, which is identified as CD34 (VI international workshop on human differentiation antigens). Its expression is a hallmark for identifying pluripotent hematopoietic stem or progenitor cells. Its expression is gradually lost as lineage committed progenitors differentiate. CD34 is a marker of choice for staining blasts in acute myeloid leukemia. In addition, it is expressed by soft tissue tumors, such as solitary fibrous tumor and gastrointestinal stromal tumor. CD34 expression is also found in vascular endothelium. Additionally, proliferating endothelial cells overexpress this molecule than the non-proliferating endothelial cells. Anti-CD34 labels > 85% of angiosarcoma and Kaposi s sarcoma, but shows low specificity.

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Anti-MAP1LC3A Mouse Monoclonal Antibody [clone: BS405]

Anti-MAP1LC3A Mouse Monoclonal Antibody [clone: BS405]

Supplier: Biosensis

MAP1A and MAP1B are microtubule-associated protein which mediate the physical interactions between microtubules and components of the cytoskeleton (probably involved in autophagosome formation). MAP1A and MAP1B each consist of a heavy chain subunit and 3 different light chain subunits (LC1, LC2 and LC3). MAP1LC3A is one of the light chain subunits and can associate with either MAP1A or MAP1B. The precursor form of MAP1LC3A is cleaved by APG4/ATG4B to form the cytosolic form LC3-1. This is activated by APG7L/ATG7, transferred to ATG3 and conjugated to phospholipid to form the membrane-bound form, LC3-II. MAP1LC3A is most abundant in heart, brain, liver, skeletal muscle and testis but is absent in thymus and peripheral leukocytes. Antibody reacts with human and rat. The antibody is expected to react with mouse MAP1LC3A protein due to 100% sequence homology.

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Pierce™ Quantitative Fluorometric Peptide Assay, Thermo Scientific

Supplier: Invitrogen

The Thermo Scientific™ Pierce™ Quantitative Fluorescent Peptide Assay is a sensitive, mix-and-read fluorescent microplate assay for the quantitative measurement of peptides and peptide mixtures.Sensitive—accurately detect as little as 5.0 µg/mL of single peptides or peptide mixturesRobust— assay performance rigorously tested using both peptides and peptide digest mixturesRobust peptide digest standard—kit includes a validated peptide digest standard for improved reproducibility of quantitationCompatible—works with many reagents, including those used in mass spectrometry sample preparationConvenient—easy mix-and-read format and stable fluorescent signal that may be read in as little as 5 minutes up to several hoursThe Pierce Quantitative Fluorescent Peptide Assay reagents include peptide assay buffer, fluorescent peptide labeling reagent, and a peptide digest assay standard for the quantitative measurement of peptide concentrations

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Ganglioside GM1 sodium salt ≥98% (by TLC)

Supplier: Adipogen

Gangliosides are acidic glycosphingolipids that form lipid rafts in the outer leaflet of the cell plasma membrane, especially in neuronal cells in the central nervous system. They participate in cellular proliferation, differentiation, adhesion, signal transduction, cell-to-cell interactions, tumorigenesis and metastasis. The accumulation of gangliosides has been linked to several diseases. Ganglioside GM1 is a major sialoglycolipid of neuronal membranes that modulates calcium homeostasis and which is important for neuronal plasticity and repair mechanisms. It binds to cholera toxin B subunit, resulting in stimulation of adenylyl cyclase in a wide variety of cell types. After cholera toxin binds to membrane associated Monosialoganglioside GM1, the A subunit of cholera toxin is translocated to the cell interior, where it catalyzes the ADP ribosylation of the membrane associated Gs subunit of adenylyl cyclase. In addition, binding of cholera toxin to monosialoganglioside GM1 causes translocation of NF-kappaB and activation of dendritic cells. E. coli heat-labile enterotoxin (LT) is structurally and functionally similar to cholera toxin and binds GM1 as well. GM1 has also been shown to improve Parkinson's disease symptoms and slow it's progression.

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Human Recombinant Enterokinase (from CHO cells)

Supplier: Peprotech

Proteases (also called Proteolytic Enzymes, Peptidases, or Proteinases) are enzymes that hydrolyze the amide bonds within proteins or peptides. Most proteases act in a specific manner, hydrolyzing bonds at, or adjacent to, specific residues, or a specific sequence of residues contained within the substrate protein or peptide. Proteases play an important role in most diseases and biological processes, including prenatal and postnatal development, reproduction, signal transduction, the immune response, various autoimmune and degenerative diseases, and cancer. They are also an important research tool, frequently used in the analysis and production of proteins. Enterokinase sequentially cleaves carboxyl side of D-D-D-D-K. Human Enterokinase is expressed as a linear 1019 amino acid polypeptide precursor glycoprotein. Proteolytic processing of this precursor generates the biologically active form of Enterokinase, which consists of two polypeptide chains (heavy chain and light chain) held together by a single disulfide bond, resulting in formation of a biologically active heterodimer. The heavy chain consists of 784 amino acid residues, and the light chain consists of 235 amino acid residues. The calculated molecular weight of Recombinant Human Enterokinase is 108.7 kDa.

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TrueBlot® Immunoprecipitation and Western Blot Kit for 6X HIS Epitope Tag, Rockland Immunochemicals

Supplier: Rockland Immunochemical

TrueBlot® Immunoprecipitation and Western Blot Kit for 6X HIS Epitope Tag

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Anti-CNN1 Mouse Monoclonal Antibody [clone: SPM169]

Supplier: Prosci

Multiple isoelectric variants of calponin have been identified, however only two molecular weight isoforms exist; a 34kDa form and a 29kDa form. Expression of the 29kDa form, I-calponin, is primarily restricted to muscle of the urogenital tract, whereas the higher molecular weight variant has been demonstrated in vascular and visceral smooth muscle. In Western blotting, this mAb reacts with only the 34kDa form of calponin in extracts of human aortic medial smooth muscle and is unreactive with fibroblast extracts of cultivated human foreskin. Calponin is a calmodulin, F-actin and tropomyosin binding protein, which is thought to be involved in the regulation of smooth muscle contraction. Calponin expression is restricted to smooth muscle cells and has been shown to be a marker of the differentiated (contractile) phenotype of developing smooth muscle.

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Anti-FN1 Mouse Monoclonal Antibody [clone: TV-1]

Supplier: Prosci

Fibronectin is a soluble dimeric glycoprotein of 440kDa, which is present in cells, extracellular matrix, and blood. There are two types of fibronectin: soluble fibronectin which is produced by hepatocytes and found in blood plasma, and insoluble cellular fibronectin which is produced by fibroblasts in a soluble form and latter assembled into an insoluble form via fibril formation.

This antibody reacts with the cellular as well as plasma form of fibronectin. Reportedly, after iv administration, this antibody localizes to tumor vessels where it binds to the underlying basement. The Fibronectin epitope recognized by this antibody is not accessible in normal tissues to the circulating antibody indicating that it can be used to specifically target tumor vessels in vivo. Clone TV-1 fibronectin antibody is reportedly useful for delivering vasoactive agents to tumors to induce increased vascular permeability or blood flow prior to treatment with chemotherapeutic drugs or antibodies.

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Anti-CEACAM5 Mouse Monoclonal Antibody [clone: C66/195]

Supplier: Prosci

This antibody recognizes proteins of 80-200kDa, identified as different members of CEA family. CEA is synthesized during development in the fetal gut and is re-expressed in increased amounts in intestinal carcinomas and several other tumors. This mAb reacts with nonspecific cross-reacting antigen (NCA) and shows a cross-reaction with human polymorphonuclear leucocytes. It shows no reaction with a variety of normal tissues and is suitable for staining of formalin/paraffin tissues. CEA is not found in benign glands, stroma, or malignant prostatic cells. Antibody to CEA is useful in detecting early foci of gastric carcinoma and in distinguishing pulmonary adenocarcinomas (60-70% are CEA+) from pleural mesotheliomas (rarely or weakly CEA+). Anti-CEA positivity is seen in adenocarcinomas from the lung, colon, stomach, esophagus, pancreas, gallbadder, urachus, salivary gland, ovary, and endocervix.

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Medium Kit without Serum and without Growth Factors, Cell Systems

Medium Kit without Serum and without Growth Factors, Cell Systems

Supplier: Cell Systems

Our suite of specialized media provides our customers with a diverse set of tools to enhance research through consistent and stable environments for cell cultures. Cell Systems media may be used with all primary, immortalized, and established cell lines.

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Anti-PPARD Rabbit Polyclonal Antibody

Anti-PPARD Rabbit Polyclonal Antibody

Supplier: Prosci

This gene encodes a member of the peroxisome proliferator-activated receptor (PPAR) family. PPARs are nuclear hormone receptors that bind peroxisome proliferators and control the size and number of peroxisomes produced by cells. PPARs mediate a variety of biological processes, and may be involved in the development of several chronic diseases, including diabetes, obesity, atherosclerosis, and cancer. This protein is a potent inhibitor of ligand-induced transcription activity of PPAR alpha and PPAR gamma. It may function as an integrator of transcription repression and nuclear receptor signaling. The expression of this gene is found to be elevated in colorectal cancer cells. The elevated expression can be repressed by adenomatosis polyposis coli (APC), a tumor suppressor protein related to APC/beta-catenin signaling pathway. Knockout studies in mice suggested the role of this protein in myelination of the corpus callosum, lipid metabolism, and epidermal cell proliferation. Alternate splicing results in multiple transcript variants.

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Orion™ Star™ A329 pH/ISE/Conductivity/Dissolved Oxygen Portable Multiparameter Meter, Thermo Scientific

Orion™ Star™ A329 pH/ISE/Conductivity/Dissolved Oxygen Portable Multiparameter Meter, Thermo Scientific

Supplier: Thermo Fisher Scientific

Accurately measure pH, ion concentration, conductivity, dissolved oxygen and temperature with the Orion™ Star™ A329 pH/ISE/Conductivity/RDO/DO Portable Meter.

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Ranger® 4000 Compact Industrial Counting Scales, OHAUS®

Ranger® 4000 Compact Industrial Counting Scales, OHAUS®

Supplier: Ohaus

Ranger® 4000 Compact Industrial Counting Scales offer the best value for durable industrial weighing and counting applications. The largest, white LED display on any scale in its class, combined with checkweighing LEDs and audible indicators, make the Ranger® 4000 highly functional in loud and dim industrial settings. The high resolution Ranger® Count 4000 has a 1:30,000 display resolution and 1:1,500,000 internal counting resolution. It also features advanced auto-optimization software which recalculates the average piece weight as the overall weight increases, ensuring accuracy and minimizing counting errors.

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GSK2126458 ≥95%

Supplier: Adipogen

GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC(50) of 0.04nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 (6nM). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110R ( E542K, E545K, and H1047R ) with Ki of 0.008nM, 0.008nM and 0.009nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.

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AV-412 ≥95%

Supplier: Adipogen

AV-412 is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In enzyme assays assay the compound inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from ABL and FLT1, which were both moderately sensitive to the compound. In cells, AV-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100nM. Moreover, AV-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.

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