PARP-1-IN-2

CAS No. 684234-55-7

PARP-1-IN-2( —— )

Catalog No. M35627 CAS No. 684234-55-7

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 149 In Stock
5MG 235 In Stock
10MG 377 In Stock
25MG 610 In Stock
50MG 869 In Stock
100MG 1152 In Stock
500MG 2313 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    PARP-1-IN-2
  • Note
    Research use only, not for human use.
  • Brief Description
    PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.
  • Description
    PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.
  • In Vitro
    PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells.PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT, increases the expression of caspase-3, caspase-9 protein and the cleaved PARP-1.Cell Proliferation Assay Cell Line:A549, HFF cellsConcentration:0, 0.1, 1, 10 μM Incubation Time:24, 48 h Result:Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells.Western Blot Analysis Cell Line:A549 cells Concentration:0, 0.1, 1, 10 μM Incubation Time:24 h Result: Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    684234-55-7
  • Formula Weight
    424.28
  • Molecular Formula
    C22H15Cl2N3O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 83.33 mg/mL (196.40 mM; Ultrasonic )
  • SMILES
    Clc1ccc(cc1)-c1nn(CC(=O)Nc2cccc(Cl)c2)c(=O)c2ccccc12
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Almahli H, et al. Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer. Bioorg Chem. 2018 Apr;77:443-456.?
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