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GNE-987

CAT: 0931-T11441-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0931-T11441-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2417371-71-0
Target
Epigenetic Reader Domain, PROTACs
Related Pathways
PROTAC, Chromatin/Epigenetic
Bioactivity
GNE-987 is a highly active chimeric BET degrader. 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 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line) .
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 Formula
C56H67F2N9O8S2
Molecular Weight
1096.31
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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