C4982
Cytochrome P450 human
3A4 isozyme microsomes, with P450 reductase and cytochrome b5, recombinant, expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
Synonym(s):
Cytochrome P450 enzyme, Human cytochrome P450, P450 enzyme
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About This Item
MDL number:
UNSPSC Code:
12161501
NACRES:
NA.47
biological source
human
Quality Level
recombinant
expressed in baculovirus infected insect cells (BTI-TN-5B1-4)
form
solution
mol wt
45-60 kDa
packaging
vial of ~0.5 nmol
vial of ≥25 units
concentration
≥2 mg/mL (Bichinchonic acid method)
technique(s)
co-immunoprecipitation (co-IP): suitable
solubility
water: soluble
suitability
suitable for molecular biology
UniProt accession no.
application(s)
cell analysis
shipped in
dry ice
storage temp.
−70°C
Gene Information
human ... CYP3A4(1576)
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General description
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.
Biochem/physiol Actions
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.
Other Notes
Microsomes containing recombinant human CYP3A4 and recombinant rabbit NADPH-P450 reductase
Unit Definition
One unit will convert 1 nanomole of testosterone to 6β-hydroxytestosterone per minute at pH 7.4 at 37 °C.
Physical form
Solution in 100 mM potassium phosphate buffer, pH 7.4.
Storage Class Code
10 - Combustible liquids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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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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