C4982
Cytochrome P450 human
3A4 isozyme microsomes, with P450 reductase and cytochrome b5, recombinant, expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
Sinónimos:
Cytochrome P450 enzyme, Human cytochrome P450, P450 enzyme
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About This Item
Número MDL:
Código UNSPSC:
12161501
NACRES:
NA.47
Productos recomendados
origen biológico
human
Nivel de calidad
recombinante
expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
Formulario
solution
mol peso
45-60 kDa
envase
vial of ~0.5 nmol
vial of ≥25 units
concentración
≥2 mg/mL (Bichinchonic acid method)
técnicas
co-immunoprecipitation (co-IP): suitable
solubilidad
water: soluble
idoneidad
suitable for molecular biology
Nº de acceso UniProt
aplicaciones
cell analysis
Condiciones de envío
dry ice
temp. de almacenamiento
−70°C
Información sobre el gen
human ... CYP3A4(1576)
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Descripción general
Research area: IMMUNO AND CKS
Cytochrome P450 (CYP450) is a membrane-bound hemoprotein that constitutes a vast superfamily of heme-thiolate proteins engaged in the metabolism of exogenous and endogenous compounds. These CYP450 enzymes feature an active heme iron center that is bound to a protein molecule via a highly conserved cysteine thiolate ligand.
Cytochrome P450 (CYP450) is a membrane-bound hemoprotein that constitutes a vast superfamily of heme-thiolate proteins engaged in the metabolism of exogenous and endogenous compounds. These CYP450 enzymes feature an active heme iron center that is bound to a protein molecule via a highly conserved cysteine thiolate ligand.
Aplicación
Cytochrome P450 human has been used in in vitro binding assays to understand protein dimerization via haem–haem stacking and its significance in cancer. It has also been used to study in vitro binding between PGRMC1 and CYP3A4.
Acciones bioquímicas o fisiológicas
Cytochrome P450 (CYP) enzymes are associated with many reactions including O-dealkylation, epoxidation, S-oxidation, and hydroxylation.
Cytochrome P450 is a heterogeneous family of isozymes whose primary function is to oxidize small molecules, both as a function of intermediary metabolism (e.g., fatty acids) and to detoxify exogenous compounds (drugs or toxins). Some isoforms have narrow substrate specificity, while others are promiscuous. The CYP1A1 isoform catalyzes 7-deethylation of ethoxyresorufin. Cytochrome P450 (CYP) plays an important role in detoxifying xenobiotics, cellular metabolism and homeostasis. One of the main mechanisms of drug-drug interactions is the induction or inhibition of these enzymes. CYP enzymes are transcriptionally activated by a variety of xenobiotics and by endogenous substrates via receptor-dependent pathways. Inhibition of these enzymes is a major factor in metabolism-based drug-drug interactions, and many chemotherapeutic medications can cause drug interactions by either inhibiting or inducing the cytochrome p450 enzyme system.
Otras notas
Microsomes containing recombinant human CYP3A4 and recombinant rabbit NADPH-P450 reductase
Definición de unidad
One unit will convert 1 nanomole of testosterone to 6β-hydroxytestosterone per minute at pH 7.4 at 37 °C.
Forma física
Solution in 100 mM potassium phosphate buffer, pH 7.4.
Código de clase de almacenamiento
10 - Combustible liquids
Clase de riesgo para el agua (WGK)
WGK 2
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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Yasuaki Kabe et al.
Cancers, 13(13) (2021-07-03)
Progesterone receptor membrane component 1 (PGRMC1) is highly expressed in various cancer cells and contributes to tumor progression. We have previously shown that PGRMC1 forms a unique heme-stacking functional dimer to enhance EGF receptor (EGFR) activity required for cancer proliferation
Andreia Palmeira et al.
Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques, 15(1), 31-45 (2012-03-01)
Aminated thioxanthones have recently been described as dual-acting agents: growth inhibitors of leukemia cell lines and P-glycoprotein (P-gp) inhibitors. To evaluate the selectivity profile of thioxanthones as inhibitors of multidrug resistance (MDR), their interaction with other ABC transporters, which were
Yasuaki Kabe et al.
Nature communications, 7, 11030-11030 (2016-03-19)
Progesterone-receptor membrane component 1 (PGRMC1/Sigma-2 receptor) is a haem-containing protein that interacts with epidermal growth factor receptor (EGFR) and cytochromes P450 to regulate cancer proliferation and chemoresistance; its structural basis remains unknown. Here crystallographic analyses of the PGRMC1 cytosolic domain
Xiangrong Zhang et al.
PloS one, 9(4), e94962-e94962 (2014-04-17)
The present study characterized in vitro metabolites of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol (20(R)-25-OCH3-PPD) in mouse, rat, dog, monkey and human liver microsomes. 20(R)-25-OCH3-PPD was incubated with liver microsomes in the presence of NADPH. The reaction mixtures and the metabolites were identified
Mirza Bojić et al.
Drug metabolism and disposition: the biological fate of chemicals, 42(9), 1438-1446 (2014-07-06)
Cilengitide is a stable cyclic pentapeptide containing an Arg-Gly-Asp motif responsible for selective binding to αVβ3 and αVβ5 integrins. The candidate drug showed unexpected inhibition of cytochrome P450 (P450) 3A4 at high concentrations, that is, a 15-mM concentration caused attenuation
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