RET-BCR Kinase Assay Service

Activity-based RET-BCR kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.

Target Overview

CAT#

-RET, BCR

Enzyme

Human BCR-RET fusion

HGNC

RET-BCR

Synonym

CDHF12, CDHR16, HSCR1, MEN2A, MEN2B, MTC1, PTC, RET51

Substrates

Peptide substrate, [RRRRRRRRRRRVYSTDYYRLFNPS], 20 µM
ATP 10 µM

Assay Properties

Reaction

Substrate + [γ-33P]-ATP = 33P-Substrate + ADP

Readout

Enzymatic activity

Reference Compound IC50s
Compounds IC50 (nM)
Staurosporine 6.2
PP2 31
AG1478 510
EGFR/ErbB Inhibitor >100,000
D-64406 140

Scientific Information

BCR; P11274 (http://www.uniprot.org/uniprot/P11274)
RET; P07949 (http://www.uniprot.org/uniprot/P07949)

Screening Location

Malvern, USA

Reference compound IC50 for RET-BCR

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