(S)-GNE-987
(S)-GNE-987 is an isomer of GNE-987 (HY-129937A), which loses VHL binding capacity and BRD4 protein degradation activity, but retains BRD4 inhibitory activity. (S)-GNE-987 is a BRD4/BET inhibitor that potently binds to the BD1 and BD2 bromodomains of BRD4, with a BRD4 BD1 IC50 of 4.0 nM and a BRD4 BD2 IC50 of 3.9 nM. (S)-GNE-987 inhibits MYC expression and exhibits inhibitory activity against acute myeloid leukemia cells, whereas its CLL1‑6 antibody-drug conjugate shows almost no in vivo antitumor efficacy in the HL‑60 xenograft tumor model. (S)-GNE-987 can be used in related research on acute myeloid leukemia.
(Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845B); Black: linker (HY-W014831)).
For research use only. We do not sell to patients.
- CAS No.: 2738533-33-8
- Formula: C56H67F2N9O8S2
- Molecular Weight:1096.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 BD1 4.0 nM (IC50) |
BRD4 BD2 3.9 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
2.0 nM
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Inhibition of cell viability in human EOL-1 acute myeloid leukemia cells.
Inhibition of cell viability in human EOL-1 acute myeloid leukemia cells.
|
31674143 |
| HL-60 | IC50 |
1.3 nM
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Inhibition of cell viability in human HL-60 acute myeloid leukemia cells.
Inhibition of cell viability in human HL-60 acute myeloid leukemia cells.
|
31674143 |
| MV4-11 | IC50 |
0.48 nM
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Inhibition of MYC expression in human MV-4-11 acute myeloid leukemia cells.
Inhibition of MYC expression in human MV-4-11 acute myeloid leukemia cells.
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31674143 |
In Vitro
(S)-GNE-987 (compound 4) inhibits the binding to the BRD4 BD1 bromodomain with an IC50 of 4.0 nM, and inhibits the binding to the BRD4 BD2 bromodomain with an IC50 of 3.9 nM[1].
(S)-GNE-987 does not inhibit binding to the VHL protein in a cell-free biochemical assay; it fails to form a stable ternary complex with BRD4 and VHL proteins in a cell-free surface plasmon resonance experiment; and it does not induce BRD4 degradation in EOL-1 acute myeloid leukemia (AML) cells[1].
(S)-GNE-987 inhibits the viability of EOL-1 acute myeloid leukemia cells with an IC50 of 2.0 nM; it inhibits the viability of HL-60 acute myeloid leukemia cells with an IC50 of 1.3 nM; it suppresses MYC expression in MV-4-11 acute myeloid leukemia (AML) cells with an IC50 of 0.48 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2738533-33-8
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Molecular Weight 1096.31
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Formula C56H67F2N9O8S2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-GNE-987 Related Classifications
HY-129937 Related Classifications
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