KRAS-related Assays: K-Ras binding assay service for compound screening and profiling using the thermal shift assay format to measure compound binding to the target
Target Overview
Target
K-Ras
HGNC
KRAS
Protein
KRAS aa 2-169, N-terminal his tag. Expressed in E. coli.
Synonyms
KRAS, C-K-RAS, CFC2, K-RAS2A, K-RAS2B, K-RAS4A, K-RAS4B, KI-RAS, KRAS1, KRAS2, NS, NS3, RASK2
Assay Properties
Scientific information
KRas: P01116 (https://www.uniprot.org/uniprot/P01116)
Screening location
Malvern, PA, US
Reaction
Compound binding to K-Ras
Readout
Protein stability change due to ligand binding via thermal shift assay
Concentration of protein in assay
The typical protein concentration in assay is 0.15 mg/ml
Concentration of compound in assay
Variable, 25 µM is recommended
Apo form Tm (°C)
50.1
Reference Compound ΔTms
| Construct | ARS-1620 | AMG-510 | BI-2852 | BAY-293 |
|---|---|---|---|---|
| Wild type | 0 | 0.5 | 0 | -0.5 |
| G12C peak 1 | 4.7 | 3.3 | 0.5 | 0.25 |
| G12C peak 2 | 12.5 | 16.5 | no 2nd peak | no 2nd peak |
| G12D | 0.5 | 0.5 | 1 | 0.5 |
| G12V | 0.25 | 0.25 | 0.75 | 0 |
Note: 0.5°C is a typical noise observed in thermal shift assay which is not significant.
Reference compound testing in thermal shift assay with K-RAS wild type and mutants
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