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C4982

Sigma-Aldrich

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

Enzyme Commission number:
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.

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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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
Haem-dependent dimerization of PGRMC1/Sigma-2 receptor facilitates cancer proliferation and chemoresistance
Kabe Y, et al.
Nature Communications, 7, 11030-11030 (2016)
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
Cytochrome P450 in Cancer Susceptibility and Treatment
Mittal B, et al.
Advances in Clinical Chemistry, 71, 77-139 (2015)
Engineering Cytochrome P450 Biocatalysts for Biotechnology, Medicine, and Bioremediation
Kumar S
Expert Opinion on Drug Metabolism & Toxicology, 6(2), 115?131-115?131 (2010)

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