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  3. GXH-II-052

GXH-II-052 

Cat. No.: HY-150684
Handling Instructions

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.

GXH-II-052 Chemical Structure

GXH-II-052 Chemical Structure

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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].

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].

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 T1/2 values of 33, 3.6 min, respectively[1].

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

Molecular Weight

1366.39

Formula

C62H76Cl2F2N14O11S2

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
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GXH-II-052
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HY-150684
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