BRAF Kinase Mutant Profiler Service

Activity-based BRAF mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#

BRAF

Enzyme

Human BRAF

HGNC

BRAF

Synonym

B-Raf proto-oncogene serine/threonine-protein kinase, B-Raf proto-oncogene serine/threonine-protein, kinase, BRAF1, RAFB1

Assay Properties
Reaction

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

Readout

Enzymatic activity

Reference Compound IC50s (nM)
Mutant Staurosporine Ro 31-8220 GW5074 H-89 Rottlerin
WT n.a. n.a. 24 n.a. n.a.
d485-489/P490Y >100,000 17,700 42 >100,000 >100,000
G464V >100,000 14,600 87 >100,000 >100,000
G469A >100,000 19,500 8.0 >100,000 >100,000
R506_K507insVLR >100,000 15,100 20 >100,000 >100,000
L597V >100,000 9,700 2.8 >100,000 >100,000
T599_V600insT >100,000 8,000 6.0 >100,000 >100,000
V599E n.a. n.a. 8.5 n.a. n.a.
V600A >100,000 8,700 3.2 >100,000 >100,000
V600D >100,000 8,800 1.7 >100,000 >100,000
V600K >100,000 7,800 2.2 >100,000 >100,000
K601E >100,000 5,800 5.0 >100,000 >100,000
FAM131B >100,000 12,000 3.7 >100,000 >100,000
KIAA1549 (Kex15Bex9) >100,000 14,700 2.3 >100,000 >100,000
KIAA1549 (Kex16Bex9) 13,000 11,300 13 >100,000 >100,000
SRGAP3 >100,000 12,500 2.7 >100,000 >100,000
Screening Location

Malvern, USA