NanoBRET Target Engagement (TE) PRMT5 Assay can be used to quantify PRMT5 binding by both peptide-substrate competitive and cofactor competitive inhibitors.
PRMT5
PRMT5
HRMT1L5, IBP72, JBP1, SKB1, SKB1Hs, HSL7, Protein arginine methyltransferase 5
HEK293 human epithelial cell line from ATCC
384-well plate format using NanoBRET TE Intracellular PRMT5 Assay
HEK293 cells transiently co-expressing NanoLuc-PRMT5 Fusion Vector and MEP50 Expression Vector were seeded into the wells of 384-well plates. The cells were pre-treated with NanoBRET Tracer PRMT5 and then treated with reference compounds LLY-283, JNJ-64619178, GSK591, EPZ015666, or GSK33326595 for 1 hour. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism program based on a sigmoidal dose response equation.
Binding of compound to target
| Compounds | IC50 (M) |
|---|---|
| LLY-283 | 7.193e-008 |
| JNJ-64619178 | 9.799e-010 |
| GSK591 | 1.962e-009 |
| EPZ015666 | 6.376e-009 |
| GSK33326595 | 1.389e-008 |
Malvern, PA, USA
More information can be found on our website Methyltransferase Assays.
Reference compound IC50 for PRMT5 + MEP50
