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 Vitro GNE-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:Solid IC50& Target:BRD4 (BD1) 4.7 nM (IC 50 ) BRD4 (BD2) 4.4 nM (IC 50 ) VHL
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
GNE-987
CAS number：2417371-71-0 molecular formula：C56H67F2N9O8S2
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2417371-71-0 | molecular formula | C56H67F2N9O8S2 |
| molecular weight | 1096.31 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
