2758117-74-5

2758117-74-5 structure

Name: PARP1/BRD4-IN-1
Chemical Name: PARP1/BRD4-IN-1
CAS Number: 2758117-74-5
Molecular Formula: C₂₉H₂₆N₆O₃
Molecular Weight: 506.56
Create Date: 2022-05-13 19:16:54
Modify Date: 2024-01-05 23:25:01
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].

Name	PARP1/BRD4-IN-1

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].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Epigenetics >> PARP Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis Signaling Pathways >> Cell Cycle/DNA Damage >> PARP Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
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]. 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]. 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.
References	[1]. Huang SH, et al. Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. Eur J Med Chem. 2022;230:114116.

Molecular Formula	C₂₉H₂₆N₆O₃
Molecular Weight	506.56

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