GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 . GNE-987 exhibits picomolar cell BRD4 degradation activity ( DC 50 =0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities ( IC 50 =4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC)In VitroGNE-987 inhibits EOL-1 and HL-60 cell viability with IC 50 s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC 50 of 0.03 nM. GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: EOL-1 cells Concentration: 0.1, 1, 10 nM Incubation Time: 5 hours Result: Degraded the BRD2 and BRD3 BET family proteins.Form:SolidIC50& Target:BRD4 (BD1) 4.7 nM (IC 50 ) BRD4 (BD2) 4.4 nM (IC 50 ) VHL. Specification: 0.99 Molecular Formula: C56H67F2N9O8S2 Molecular Weight: 1096.31 PubChem CID: 145925661
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- G649187-5mg
- CAS:
- 2417371-71-0
- Product Size:
- 5mg
