1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
    c-Myc
    Caspase
  3. PROTAC BRD4 Degrader-6

PROTAC BRD4 Degrader-6 

Cat. No.: HY-131203
Handling Instructions

PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research.

For research use only. We do not sell to patients.

PROTAC BRD4 Degrader-6 Chemical Structure

PROTAC BRD4 Degrader-6 Chemical Structure

CAS No. : 2410947-56-5

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Description

PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research[1].

IC50 & Target[1]

BRD4 BD1

2.7 μM (IC50)

Caspase 3

 

In Vitro

PROTAC BRD4 Degrader-6 (compound 32a) (72 hours; BxPC3 cell) has anti-proliferation activity with IC50 value of 0.165 μM[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces BRD4 protein degradation in a time-dependent manner, which results in the continuous decrease of c-Myc expression[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces the cell cycle arrest and apoptosis[1].

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

Western Blot Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: Degraded BRD4 protein in a time-dependent manner and inhibits the expression of c-Myc.

Cell Cycle Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: Increase in G0/G1 and G2/M phase cells, and a decrease of S phase cells.

Apoptosis Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: The percentage of cells in early and late apoptosis was recorded as 10.10% and 12.36%, respectively.

Western Blot Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: The expression of caspase 3 and cleaved-caspase 3 significantly increased.
Molecular Weight

926.90

Formula

C43H40F2N10O10S

CAS No.
SMILES

O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5

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Storage

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

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PROTAC BRD4 Degrader-6
Cat. No.:
HY-131203
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