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

PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability.

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PARP-2-IN-3 Chemical Structure

PARP-2-IN-3 Chemical Structure

CAS No. : 2915650-86-9

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Description

PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability[1].

IC50 & Target[1]

PARP-2

0.07 μM (IC50)

In Vitro

PARP-2-IN-3 (Compound 12) (24 h) shows cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively[1].
PARP-2-IN-3 (6.05 μM; 24 h) arrests cell cycle at G2/M phase, and induces apoptosis and necrosis in MCF-7 cells[1].
PARP-2-IN-3 fills the space inside the PARP-2 pocket in a manner similar to Olaparib (HY-10162)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 and MCF-7
Concentration:
Incubation Time: 24 h
Result: Displayed remarkable cytotoxic activities with IC50s of 6.14±0.5 μM and 6.05±0.4 μM against MDA-MB-231 and MCF-7, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 6.05 μM
Incubation Time: 24 h
Result: The percentage of cells in pre-G1 phase increased from 1.85% to 33.47%, while in G2/M phase increased from 11.84% to 32.04%. The percentage of cells in S phase slightly decreased from 29.95% to 26.18% and in G0/G1 phase decreased from 58.21% to 41.78%.

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 6.05 μM
Incubation Time: 24 h
Result: Induced an early apoptotic effect 22.52% and late apoptotic effect 3.72% in comparison to the untreated negative control MCF-7 cells which induced an early and late apoptotic effect 0.37% and 0.33%, respectively.
Molecular Weight

385.84

Formula

C20H20ClN3O3

CAS No.
SMILES

O=C(NC1=CC=C(C2=NC3=CC(Cl)=CC=C3O2)C=C1)CCN4CCOCC4

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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PARP-2-IN-3 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PARP-2-IN-3
Cat. No.:
HY-151625
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