GNE-987
Product Specifications
UNSPSC Description
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=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 (IC50=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)[1].
Target Antigen
Epigenetic Reader Domain; PROTACs
Type
Reference compound
Related Pathways
Epigenetics;PROTAC
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gne-987.html
Purity
99.91
Solubility
DMSO : 150 mg/mL (ultrasonic)
Smiles
O=C([C@H](C[C@@H](O)C1)N1C([C@@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7
Molecular Weight
1096.31
References & Citations
[1]Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, stored under nitrogen)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-129937A/GNE-987-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-129937A/GNE-987-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
2417371-71-0
Available Sizes
Curated Selection
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