1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. PARP
    Apoptosis
  3. PARP1-IN-12

PARP1-IN-12 

Cat. No.: HY-150765
Handling Instructions

PARP1-IN-12 is a potent PARP1 inhibitor with IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells.

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

PARP1-IN-12 Chemical Structure

PARP1-IN-12 Chemical Structure

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Description

PARP1-IN-12 is a potent PARP1 inhibitor with IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells[1].

IC50 & Target

PARP-1

2.99 nM (IC50)

In Vitro

PARP1-IN-12 (compound 20e) (0.1, 0.3, 1 µM; 48 h) exhibits activities of antiproliferation and selectively killing BRCA-deficient cells, can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells in a concentration-dependent manner[1].
PARP1-IN-12 (10 µM, 48 h) enhances the protein levels of phosphorylated Chk1[1].
PARP1-IN-12 (1, 3, 10 µM; 48 h) activats cell cycle checkpoints, then induces G2/M arrest in BRCA-deficient cells and (1, 5, 10 µM; 96 h) also induces MDA-MB-436 cells apoptosis in a concentration-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: UWB1.289 (BRCA1-deficient), UWB1.289+BRCA1 (BRCA1 restored), MDA-MB-436 (BRCA1-deficient), Capan-1 (BRCA2-deficient) cells
Concentration: 0.1, 0.3, 1 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity with IC50s of 0.27, 1.43, 0.87, 0.19 µM for UWB1.289, UWB1.289+BRCA1, Capan-1 and MDA-MB-436 cells, respectively.

Immunofluorescence[1]

Cell Line: MDA-MB-436, Capan-1 cells
Concentration: 10 µM
Incubation Time: 48 h
Result: Enhanced the protein levels of phosphorylated Chk1 but the levels of corresponding total proteins were not altered.

Cell Cycle Analysis[1]

Cell Line: Capan-1 cells
Concentration: 1, 3, 10 µM
Incubation Time: 48 h
Result: Induced G2/M arrest in BRCA-deficient cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 1, 5, 10 µM
Incubation Time: 96 h
Result: Caused apoptosis in a concentration-dependent manner in MDA-MB-436 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-436, Capan-1 cells
Concentration: 0.1, 0.3, 1 µM
Incubation Time: 48 h
Result: Induced increased levels of γH2AX in a concentration-dependent manner in both MDA-MB-436 and Capan-1 cells.
Molecular Weight

741.93

Formula

C43H56FN5O5

SMILES

FC1=CC=C(CC(C2C=CC=CC23)=NNC3=O)C=C1C(N4CCN(CC4)C(CCCCCCCNCC5C(OC6C5C=C7[[email protected]@](C)(C6)CCC[[email protected]@H]7C)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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PARP1-IN-12
Cat. No.:
HY-150765
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