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High Throughput P450 Inhibition Kits

High Throughput P450 Inhibition Kits

These human Cytochrome P450 High Throughput Inhibitor Screening Kits are designed to rapidly screen for potential inhibitors of Cytochrome P450 catalytic activity. Each kit provides all the necessary components and instructions for measuring the IC50 value of up to 38 test compounds in 96-well plates. The inhibitor screening kit includes the following components: recombinant human P450, (Supersomes™ Enzymes) fluorescent P450 substrate, positive control inhibitor, metabolite standard, NADPH regenerating system, reaction buffer, stop reagent, control membrane protein, and an instruction manual.

Follow this link to learn more about high throughput screening methodology for human cytochrome P450 inhibition. This link will provide a detailed method for those who want to use the individual components supplied by BD Biosciences to run their High Throughput Assays. This bulletin describes the methodology for CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 assays.

CYP3A4/BFC - Cat. No. 459100 (formerly HTS-1000)
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2C8/DBF - Cat. No. 459320
Product data sheet
Instruction Manual
Supplemental Instructions
CYP3A4/BQ - Cat. No. 459110
Product data sheet
Instruction Manual
Supplemental Instructions

CYP2C9/MFC - Cat. No. 459300 (formerly HTS-3000)
Product data sheet
Instruction Manual
Supplemental Instructions

CYP3A4/DBF - Cat. No. 459120
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2C19/CEC - Cat. No. 459400 (formerly HTS-4000)
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2D6/AMMC - Cat. No. 459200 (formerly HTS-2000)
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2A6/Coumarin - Cat. No. 459420
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2B6/EFC - Cat. No. 459220
Product data sheet
Instruction Manual
Supplemental Instructions
CYP2E1/MFC - Cat. No. 459620
Product data sheet
Instruction Manual
Supplemental Instructions
CYP19/MFC - Cat. No. 459520
Product Information
Product data sheet
Instruction Manual
Supplemental Instructions
CYP1A2/CEC - Cat. No. 459500
Product data sheet
Instruction Manual
Supplemental Instructions

Final HTS Kit Assay Concentrations
Based on reaction volume of 200 µL/well
HTS P450 Inhibition Kit
Catalog No.
Enzyme (pmol/well)
Substrate (µM)
NADP+ (µM)
Glucose-6-Phosphate (mM)
Magnesium Chloride
Hexahydrate (mM)
Glucose-6-Phosphate Dehydrogenase (Units/mL)
3A4/BFC
459100
1
50
8.1
0.4
0.4
0.2
3A4/BQ
459110
1.5
40
8.1
0.4
0.4
0.2
3A4/DBF
459120
0.2
1
8.1
0.4
0.4
0.2
2D6/AMMC
459200
1.5
1.5
8.1
0.4
0.4
0.2
2C8/DBF
459320
1.8
1
8.1
0.4
0.4
0.2
2C9/MFC
459300
1
75
8.1
0.4
0.4
0.2
2C19/CEC
459400
1
25
8.1
0.4
0.4
0.2
2A6/Coumarin
459420
1
3
8.1
0.4
0.4
0.2
1A2/CEC
459500
1
5
8.1
0.4
0.4
0.2
2B6/EFC
459220
1
2.5
8.1
0.4
0.4
0.2
2E1/MFC
459620
1
70
8.1
0.4
0.4
0.2

96 Well Assay Plates
For all fluorescent P450 assays we recommend the BD Falcon 96 well black plates (Cat. No. 353241(25/pk, 100/cs)) and lids (Cat. No. 353958). These plates are not a component of the Gentest P450 Inhibition kits and must be purchased separately.

Please note these products are available through your Fisher or VWR representative.
The equivalent catalog number for these vendors are:
Fisher 96 well black plates (Cat. No. 02-683-140) and lids (Cat. No. 08-772-113).
VWR 96 well black plates (Cat. No. 22221-572) and lids (Cat. No. 62406-486).

BD Biosciences