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GXH-II-052

Product Specifications

UNSPSC Description

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[1].

Target Antigen

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gxh-ii-052.html

Solubility

10 mM in DMSO

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

Molecular Weight

1366.39

References & Citations

[1]Guan X, et al. Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. J Med Chem. 2022 Jul 22.

Shipping Conditions

Room temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-150684/GXH-II-052-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-150684/

Clinical Information

No Development Reported

CAS Number

3031654-49-3

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