PARP-2-IN-3

CAS No. 2915650-86-9

PARP-2-IN-3( —— )

Catalog No. M36489 CAS No. 2915650-86-9

PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.CAS ??128-52-56-8

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PARP-2-IN-3
  • Note
    Research use only, not for human use.
  • Brief Description
    PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.CAS ??128-52-56-8
  • 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.
  • 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.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.PARP-2-IN-3 fills the space inside the PARP-2 pocket in a manner similar to Olaparib (HY-10162).Cell Cytotoxicity Assay 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 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 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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP | Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2915650-86-9
  • Formula Weight
    385.84
  • Molecular Formula
    C20H20ClN3O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(NC=1C=CC(=CC1)C2=NC3=CC(Cl)=CC=C3O2)CCN4CCOCC4
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. El-Ghobashy NM, et al. Synthesis, biological evaluation, and molecular modeling studies of new benzoxazole derivatives as PARP-2 inhibitors targeting breast cancer. Sci Rep. 2022 Sep 28;12(1):16246.?
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