GXH-II-052
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.
For research use only. We do not sell to patients.
- CAS No.: 3031654-49-3
- Formula: C62H76Cl2F2N14O11S2
- Molecular Weight:1366.39
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD4-1 28 nM (Kd) |
BRD4-2 9.1 nM (Kd) |
BRD4-T 4.8 nM (Kd) |
BRDT-1 0.6 nM (Kd) |
BRDT-2 8.4 nM (Kd) |
BRDT-T 2.6 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| MM1.S | IC50 |
59 nM
Compound: GXH-II-0652
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Growth inhibition of human MM1.S cells incubated for 72 hrs by CellTiter-Blue assay
Growth inhibition of human MM1.S cells incubated for 72 hrs by CellTiter-Blue assay
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[PMID: 35867655] |
GXH-II-052 (0-10 μM; 72 h) shows antiproliferative activity with an IC50 value of 59 nM in MM1.S cells[1].
GXH-II-052 (0-10 μM; 6 h) decreases the expression of c-Myc in a dose dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1.S cells
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed growth inhibition with an IC50 value of 59 nM in multiple myeloma MM1.S cells.
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Cell Line:MM1.S cells
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Concentration:0-10 µM
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Incubation Time:6 h
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Result:Decreased the expression of c-Myc in a dose dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3031654-49-3
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Molecular Weight 1366.39
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Formula C62H76Cl2F2N14O11S2
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SMILES
O=C(N1CCC(NC(C2=CC=C(NC3=NC=C(C)C(NC4=CC=C(Cl)C(NS(=O)(C(C)(C)C)=O)=C4)=N3)C=C2F)=O)CC1)COCCOCCOCC(N5CCC(NC(C6=CC=C(NC7=NC=C(C)C(NC8=CC=C(Cl)C(NS(=O)(C(C)(C)C)=O)=C8)=N7)C=C6F)=O)CC5)=O
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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)
GXH-II-052 Related Classifications
HY-150684 Related Classifications
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