2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP Apoptosis
  4. 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

PARP-2-IN-3 Chemical Structure

CAS No. : 2915650-86-9

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Based on 1 publication(s) in Google Scholar

PARP-2-IN-3 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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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)

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
6.05 μM
Compound: 175a
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 38838546]
MDA-MB-231 IC50
6.14 μM
Compound: 175a
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 38838546]
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.html" class="link-product" target="_blank">Olaparib (HY-10162)[1].

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

PARP-2-IN-3 Related Antibodies

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
Shipping

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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Help & FAQs
  • 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.

Keywords:

PARP-2-IN-32915650-86-9PARPApoptosispoly ADP ribose polymerase breast cancerMCF-7MDA-MB-231Inhibitorinhibitorinhibit

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