Activity-based ERN1 (R727A) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
ERN1/IRE1 (R727A)
Enzyme
Human ERN1/IRE1 (R727A)
HGNC
ERN1 (R727A)
Synonym
Serine/threonine-protein kinase/endoribonuclease IRE1, Endoplasmic reticulum-to-nucleus signaling 1, Inositol-requiring protein 1
Substrates
MBP (Myelin Basic Protein), 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 | 37 |
| Ro 31-8220 | 7,500 |
| GW5074 | 1,600 |
| H-89 | >100,000 |
| Rottlerin | >100,000 |
Scientific Information
O75460 (http://www.uniprot.org/uniprot/O75460)
Screening Location
Malvern, USA
Reference compound IC50 for ERN1/IRE1 (R727A)
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