1. Cell Cycle/DNA Damage
    Epigenetics
    PI3K/Akt/mTOR
    Apoptosis
  2. PARP
    PI3K
    Apoptosis
  3. PARP/PI3K-IN-1

PARP/PI3K-IN-1 

Cat. No.: HY-133124
Handling Instructions

PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.

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

PARP/PI3K-IN-1 Chemical Structure

PARP/PI3K-IN-1 Chemical Structure

CAS No. : 2337386-47-5

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Description

PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases[1].

IC50 & Target

PARP-1

8.22 (pIC50)

PARP-2

8.44 (pIC50)

PI3Kα

8.25 (pIC50)

PI3Kβ

6.54 (pIC50)

PI3Kδ

8.13 (pIC50)

PI3Kγ

6.08 (pIC50)

In Vitro

PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis[1].
PARP/PI3K-IN-1 (1 μM; 72 hours) reduces the autophosphorylation levels of AKT and S6 while increases the autophosphorylation level of ERK after treating cells, indicating that it can inhibit the PI3K pathway and activate the ERK pathway[1].
PARP/PI3K-IN-1 (1 μM) displays a strong capability to downregulate the expression of BRCA1/2 at the mRNA level in MDA-MB-468 cancer cells[1].
PARP/PI3K-IN-1 not only shows significant inhibitory activity against BRCA-deficient cells HCC1937 and HCT116, but also displays potent anti-proliferative activity against BRCA-proficient cells MDA-MB-231 and MDA-MB-468[1].

Apoptosis Analysis[1]

Cell Line: MDA-MB-468 cancer cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Led to a significant increase in cell apoptosis.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cancer cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Reduced the autophosphorylation levels of AKT and S6 while increased the autophosphorylation level of ERK after treating cells.
In Vivo

PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth[1].

Animal Model: Six-week-old male BALB/c nude mice with MDA-MB-468 cells[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily (BID) for 34 consecutive days
Result: Significantly suppressed the tumor growth.
Molecular Weight

660.62

Formula

C₃₃H₂₈F₄N₈O₃

CAS No.

2337386-47-5

SMILES

O=C1NN=C(CC2=CC=C(F)C(C(N3CCC4=C(N5CCOCC5)N=C(C6=C(C(F)(F)F)C=C(N)N=C6)N=C4C3)=O)=C2)C7=C1C=CC=C7

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

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Keywords:

PARP/PI3K-IN-1PARPPI3KApoptosispoly ADP ribose polymerase Phosphoinositide 3-kinaseAnticanceroncologicanti-proliferativeBRCA1-deficientbreastcancercolorectaltriple-negativeInhibitorinhibitorinhibit

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