Assays & Kits

Vascular endothelial growth factor receptor 2 (VEGFR2), also called Kinase insert Domain receptor (KDR), is a tyrosine kinase (TK) receptor for VEGFs that plays a central role in tumor angiogenesis; therefore the inhibition of VEGFR2 is a promising therapeutic strategy for inhibiting angiogenesis and tumor growth. The VEGFR2 Kinase Assay Kit is designed to measure VEGFR2 kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent.

The epidermal growth factor receptor (EGFR; ErbB-1; HER1) is the cellsurface receptor for members of the epidermal growth factor family. Overexpression and/or hyperactivation of EGFR kinase is associated with several human cancers such as lung, glioblastoma, and epithelian tumors of the neck and head, leading to the development of anticancer therapeutics targeting EGFR. T790M, L858R and C797S mutations in EGFR cause resistance to known EGFR inhibitors. The EGFR(T790M/C797S/L858R) Kinase Assay Kit is designed to identify mutant-selective EGFR kinase inhibitors and to measure EGFR (T790M/C797S/L858R) kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent.

The SMARCA4 TR-FRET Assay Kit is designed to measure the inhibition of SMARCA4 binding to its substrate in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing terbium-labeled donor, dye-labeled acceptor, SMARCA4, substrate, and an inhibitor is incubated for 120 minutes. Then, the fluorescence intensity is measured using a fluorescence reader.

The SMARCA2 TR-FRET Assay Kit is designed to measure the inhibition of SMARCA2 (BRM) binding to its substrate in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing terbium-labeled donor, dye-labeled acceptor, SMARCA2, substrate, and an inhibitor is incubated for 120 minutes. Then, the fluorescence intensity is measured using a fluorescence reader.

HER2 (human epidermal growth factor receptor 2) encoded by ERBB2 gene has been found to be overexpressed in certain aggressive breast cancers, suggesting it as an important drug target as well as a biomarker. The HER2 Kinase Assay Kit is designed to measure HER2 kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent.

The FAK Kinase Assay Kit is designed to measure FAK kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent.

B-raf, after stimulation by activated RAS, phosphorylates MEK1 resulting in activation of the mitogen-activated protein (MAP) kinase cascade. Since the MAPK cascade has been shown to be a critical factor in melanoma development, it has been proposed that targeting B-raf could be a promising approach to combat melanoma. More importantly, 40-60% of melanomas display a mutation in BRAF, e.g. B-Raf(V600E), which leads to constitutive activation of the MAP kinase pathway. The B-Raf(V600E) Kinase Assay Kit is designed to measure B-Raf(V600E) kinase activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent. In addition, the B-Raf(V600E) Kinase Assay Kit includes wild type B-Raf enzyme as a positive control for researchers investigating B-Raf(V600E) specific inhibitors.

The Sirtuin 6 Fluorogenic Assay Kit is a complete assay system designed to measure SIRT6 activity for screening and profiling applications. It comes in a convenient 96-well format, with all the reagents necessary for 100 fluorescent SIRT6 activity measurements. In addition, the kit includes purified SIRT6 enzyme and a SIRT inhibitor, Nicotinamide, for use as a positive and negative control, respectively. The Fluorogenic SIRT6 Assay Kit is based on a unique fluorogenic substrate and developer combination. This assay method eliminates dealing with the radioactivity, extraction, and chromatography aspects of traditional assays. Using this kit, only two simple steps on a microtiter plate are needed to analyze the SIRT6 activity level. First, the Sirtuin 6 fluorometric substrate, containing a myristoylated lysine side chain, is incubated with purified SIRT6 enzyme. The demyristoylation sensitizes the substrate so subsequent treatment with the SIRT Developer produces a fluorophore that can t

HDAC assay developer is an essential reagent for signal generation in HDAC assays performed with any of BPS Bioscience's HDAC fluorimetric substrates or assay kits. An appropriate fluorimetric substrate, comprising an acetylated lysine side chain, is first incubated with a sample containing HDAC activity (nuclear or cellular extract, purified enzyme, bead-bound immunocomplex, etc.). Deacetylation of the substrate sensitizes it so that, in a second step, treatment with the HDAC assay developer produces a fluorophore. Trichostatin A is included as an 'inhibitor stop' for class I and II HDACs.