C4982
Cytochrome P450 human
3A4 isozyme microsomes, with P450 reductase and cytochrome b5, recombinant, expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
Synonyme(s) :
Cytochrome P450 enzyme, Human cytochrome P450, P450 enzyme
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About This Item
Numéro MDL:
Code UNSPSC :
12161501
Nomenclature NACRES :
NA.47
Produits recommandés
Source biologique
human
Niveau de qualité
Produit recombinant
expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
Forme
solution
Poids mol.
45-60 kDa
Conditionnement
vial of ~0.5 nmol
vial of ≥25 units
Concentration
≥2 mg/mL (Bichinchonic acid method)
Technique(s)
co-immunoprecipitation (co-IP): suitable
Solubilité
water: soluble
Adéquation
suitable for molecular biology
Numéro d'accès UniProt
Application(s)
cell analysis
Conditions d'expédition
dry ice
Température de stockage
−70°C
Informations sur le gène
human ... CYP3A4(1576)
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Description générale
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.
Application
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.
Actions biochimiques/physiologiques
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.
Autres remarques
Microsomes containing recombinant human CYP3A4 and recombinant rabbit NADPH-P450 reductase
Définition de l'unité
One unit will convert 1 nanomole of testosterone to 6β-hydroxytestosterone per minute at pH 7.4 at 37 °C.
Forme physique
Solution in 100 mM potassium phosphate buffer, pH 7.4.
Code de la classe de stockage
10 - Combustible liquids
Classe de danger pour l'eau (WGK)
WGK 2
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
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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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