2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis DNA/RNA Synthesis PARP
  4. Polθ/PARP-IN-1

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity.

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Polθ/PARP-IN-1 Chemical Structure

Polθ/PARP-IN-1 Chemical Structure

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Polθ/PARP-IN-1 Related Antibodies

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Description

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity[1].

In Vitro

Polθ/PARP-IN-1 (compound 25d) (0-80 µM; 3 days) shows antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 µM for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively[1].
Polθ/PARP-IN-1 (compound 25d) (2 µM; 3 days) induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage[1].

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

Polθ/PARP-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells
Concentration: 0-80 µM
Incubation Time: 5 days
Result: Showed antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 µM for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 2 µM
Incubation Time: 3 days
Result: Induced apoptosis with a higher apoptosis rate (26.7%) and arrested cell cycle progression at the G2/M phase.
In Vivo

Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; daily for 21 consecutive days) inhibits tumor growth in MDA-MB-436 xenograft model[1].

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

Animal Model: 18-20 g, Six-week-old female BALB/C nude mice (MDA-MB-436 xenograft model)[1]
Dosage: 20, 40 mg/kg
Administration: I.p.; daily for 21 consecutive days
Result: Significantly inhibited the growth of MDA-MB-436 xenografts in a dose-dependent manner, exerted an optimal inhibitory potency with a tumor growth inhibition (TGI) rate of 54.4%, 74.7% at 20, 40 mg/kg, respectively.
Molecular Weight

754.23

Formula

C38H33ClFN7O5S
SMILES

COC1=CC=C(C=C1C2=CC(C)=NC=C2C(NC3=NN=C(S3)OCC4CCN(CC4)C(C5=C(C=CC(CC6=NNC(C7=C6C=CC=C7)=O)=C5)F)=O)=O)Cl
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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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Polθ/PARP-IN-1 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:

Polθ/PARP-IN-1ApoptosisDNA/RNA SynthesisPARPpoly ADP ribose polymeraseMDA-MB-436 cellsanti-cancerG2/M phaseapoptosisantiproliferativeInhibitorinhibitorinhibit

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