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Key Documents

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)

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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

UniProt accession no.

application(s)

cell analysis

shipped in

dry ice

storage temp.

−70°C

Gene Information

human ... CYP3A4(1576)

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Biochem/physiol Actions

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.

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

10 - Combustible liquids

wgk_germany

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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