GXH-II-052

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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 K_d 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.

GXH-II-052 Chemical Structure

CAS No. : 3031654-49-3

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Description

IC₅₀ & Target^[1]

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)

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	MM1.S cells
Concentration:	0-10 µM
Incubation Time:	72 h
Result:	Showed growth inhibition with an IC₅₀ value of 59 nM in multiple myeloma MM1.S cells.

Western Blot Analysis^[1]

Cell Line:	MM1.S cells
Concentration:	0-10 µM
Incubation Time:	6 h
Result:	Decreased the expression of c-Myc in a dose dependent manner.

In Vivo

GXH-II-052 shows metabolic stability in mouse and human liver microsomes with an T_1/2 values of 33, 3.6 min, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1366.39

Formula

C₆₂H₇₆Cl₂F₂N₁₄O₁₁S₂

CAS No.

3031654-49-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

GXH-II-052 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GXH-II-0523031654-49-3Epigenetic Reader Domainantiproliferativec-MycMM1.S cellsmetabolic stabilityInhibitorinhibitorinhibit

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