pathELECT^℠ Personalized Screening & Profiling

pathELECT provides you access to a growing menu of novel biosensor assays that monitor multiple stages of cell signaling to determine whether a target protein degrades, translocates or is secreted. Screen or profile your compounds against one of our functional whole cell pathway signaling assays. pathELECT is a simple and cost-effective alternative to in-house profiling and screening and is ideal for any size compound collection, providing you a flexible solution for hit identification and ongoing lead optimization & SAR.

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Panel Features & Benefits

Single functional readout – applicable to different kinase receptors and families
Stable cell lines - increased reliability and reproducibility
All cell lines functionally validated to ensure high-quality results every time
High specificity – tagged protein eliminates background from endogenous proteins
High quality reproducible data – superior assay windows & robust performance (Z' > 0.6)

How it Works

Screen for Activators or Inhibitors of PI3-K/AKT Signalling

PathHunter® assays are able to measure FOXO translocation in response to PI3 or AKT inhibition.

pathELECT Assay Panel

Listed below are the assays currently available for screening and profiling.

Target Gene ▲	Common Name	Family	Accession No.
BCL2-BAX	BCL2 B-cell CLL/lymphoma 2 (Bcl-2)	BCL2	NM_000633
BCL2-BIM	BCL2 B-cell CLL/lymphoma 2 (Bcl-2)	BCL2	NM_000633
BCL2L1-BAX	BCL2-like 1 (Bcl-xL)	BCL2	NM_138578.1
BCL2L1-BIM	BCL2-like 1 (Bcl-xL)	BCL2	NM_138578.1
CDC25A	Cell division cycle 25 homolog A (CDC25A)	Cell Cycle Protein	NM_001789.2
FOXO3	forkhead box O3 (forkhead box O3)	Pathway	NM_001455
IκB	nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (NFKBIA)	Pathway	NM_020529
Keap1-NRF2	nuclear factor (erythroid-derived 2)-like 2 (NFE2L2)	Transcription Factor	NM_006164
MCL1-BIM	Myeloid cell leukemia sequence 1 (Mcl-1)	BCL2	NM_021960
NIK	mitogen-activated protein kinase kinase kinase 14 (NIK)	STE	NP_003945.2
NPR1	Natriuretic peptide receptor A (NPR1)	Guanylate Cyclase A	NM_000906.3
P53	P53 (P53)	Nuclear Translocation	NM_000546.2
RANK-IκB	Tumor necrosis factor receptor superfamily, member 11a (TNFRSF11A)	Tumor Necrosis Factor Receptor Superfamily	NM_003839.3
RELA-IκB	v-rel reticuloendotheliosis viral oncogene homolog A (avian) (RELA)	Transcription factor	NM_021975
SREBP2	Sterol regulatory element binding transcription factor 2 (SREBF2)	Transcription Factor	NM_004599.2
TORC1	CREB regulated transcription coactivator 1 (CRTC1)	Transcription factor	NM_015321.1
TORC2	CREB regulated transcription coactivator 2 (CRTC2)	Transcription factor	NM_181715
XBP1	X-box binding protein 1 (XBP1)	Transcription factor	BC012841
β-Catenin	Catenin (cadherin-associated protein), beta 1 (CTNNB1)	Wnt-Frizzled signalling	NM_001904

Data Analysis & Interpretation

Definitions

Percent Activity/Inhibition

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:

% Activity
(Agonist Mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

% Inhibition
(Antagonist mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity)

Dose Response Curve (EC50/IC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:

pathELECT℠ Personalized Screening & Profiling