1. Epigenetics
    Cell Cycle/DNA Damage
    Apoptosis
  2. Epigenetic Reader Domain
    PARP
    Apoptosis
    DNA/RNA Synthesis
  3. PARP1/BRD4-IN-1

PARP1/BRD4-IN-1 

Cat. No.: HY-144338
Handling Instructions

PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.

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

PARP1/BRD4-IN-1 Chemical Structure

PARP1/BRD4-IN-1 Chemical Structure

CAS No. : 2758117-74-5

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Description

PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells[1].

IC50 & Target

BRD4

202 nM (IC50)

PARP1

49 nM (IC50)

In Vitro

PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1 and G2/M phase in SW1990 cells[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells[1].

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

Cell Proliferation Assay

Cell Line: CFPAC-1, SW1990, MDA-MB-231, MDA-MB-468, HCT-116, THP-1[1]
Concentration: 0-2 μM
Incubation Time: 3, 4 or 7 days
Result: Showed potent inhibition of the growth of cancer cell lines.

Western Blot Analysis

Cell Line: SW1990[1]
Concentration: 0, 1, 2 μM
Incubation Time: 4 days
Result: Significantly inhibited the expression of PARP1 and BRD4 at 2 μM.

Cell Cycle Analysis

Cell Line: SW1990[1]
Concentration: 1, 2 μM
Incubation Time: 4 days
Result: Arrested the cell cycle at G0/G1 and G2/M phase.

Apoptosis Analysis

Cell Line: SW1990[1]
Concentration: 0, 1, 2 μM
Incubation Time: 4 days
Result: Showed potent efficacy on the apoptosis of SW1990 cells at 2 μM.
In Vivo

PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice[1].

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

Animal Model: Athymic nude mice (6-7 weeks, 18-20 g, SW1990-injected)[1]
Dosage: 30mg/kg
Administration: Intraperitoneal injection for 28 days
Result: Significantly inhibited the tumor size and weight and did not cause significant damage of the kidney, lung, spleen, liver and heart.
Molecular Weight

506.56

Formula

C29H26N6O3

CAS No.
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Storage

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

References
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Product Name:
PARP1/BRD4-IN-1
Cat. No.:
HY-144338
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