PARP1/BRD4-IN-1 

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].

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].

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

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].

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

506.56

C₂₉H₂₆N₆O₃

2758117-74-5

O=C(C1=CC=CC2=C1NC(CN3C(N(C)C4=CC=C(C5=C(C)ON=C5C)C=C4C3C6=CC=CC=C6)=O)=N2)N

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]