Iniparib (BSI-201) 化学構造
分子量: 292.03



Quality Control & MSDS


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情報 Iniparib (BSI-201)は、推定のPoly(ADPリボース)ポリメラーゼ(PARP I)阻害剤です
In vitro試験 BSI-201 is described as a prodrug of 4-iodo-3-nitrosobenzamide, an agent that covalently inhibits PARP1 by binding to its first zinc finger under cell-free conditions. Treatment of 120 μM BSI-201 plus buthionine sulfoximine (BSO) induces a 95% cell death among 855-2 cells, and displays a similar effect in other human cancer cells. [1] BSI-201 inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. [2] Recently BSI-201 shows no ability to inhibit PARP enzymatic or cellular activity, but can non-selectively modify cysteine-containing proteins in tumor cells, suggesting the mechanism of action for BSI-201 is likely not via inhibition of PARP activity. [3] BSI-201 (100 μM) inhibits ionizing radiation-induced single-strand breaks (SSBs) repair in human lymphoid cell lines based on large endogenous Epstein–Barr virus (EBV) circular episomes assay, resulting in 55% repair by 2 hours, which can be reversed surprisingly by knockdown of PARP1, indicating that the mechanism of inhibition does not involve trapping PARP at SSBs. [4] BSI-201 is not able to selectively kill homologous recombination (HR)-deficient cells between BRCA2-deficient PEO1 and BRCA2-revertant PEO4, or ATM-deficient GM16666 and ATM-restored GM16667 fibroblasts. BSI-201 is cytotoxic to a variety of cell lines at concentrations above 40 μM reflecting a mechanism independent of PARP. [5]
In vivo試験

推薦された実験操作 (公開の文献だけ)

細胞アッセイ: [3]

細胞系 MDA-MB-231, and MDA-MB-436
濃度 Dissolved in DMSO, final concentrations ~10 μM
処理時間 5, and 9 days
方法 Cells are exposed to various concentrations of BSI-201 for 5, and 9 days in the presence or absence of buthionine sulfoxamide (BSO). After treatment, cell proliferation is measured by CellTiter-Glo assay.



Download Iniparib (BSI-201) SDF
分子量 292.03


CAS No. 160003-66-7
別名 SAR240550
溶解度 (25°C)
  • DMSO 58 mg/mL
  • 水 <1 mg/mL
  • エタノール 28 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 4-iodo-3-nitrobenzamide


カスタマーレビュー (2)

Click to enlarge
Source , , Nat Methods, 2013, 10(10):981-4. Iniparib (BSI-201) purchased from Selleck
Method Immunoblot analysis
Cell Lines HCT116
Concentrations 50 uM
Incubation Time 40 min
Results Immunoblot analysis of PARylation after treatment with AIniparib.The asterisk indicates a nonspecific band.

Click to enlarge
Source Neuroscience, 2010, 171, 1256–1264. Iniparib (BSI-201) purchased from Selleck
Method Western blot
Cell Lines Wt neurons
Concentrations 25 μM
Incubation Time 24 h
Results Our results indicate that TWEAK induces NF-κB activation in neurons and that this effect is abrogated by PARP-1 inhibitor BSI-201 (Fig. E). Wt neurons were incubated with TWEAK alone or in combination with BSI-201 followed by a Western blot analysis with an antibody that detects cleaved caspase-3. We found that TWEAK induces caspase-3 cleavage and that this effect is attenuated by PARP-1 inhibitor BSI-201 (Fig. F)

製品表彰状 (2)

  • Site-specific characterization of the Asp- and Glu-ADP-ribosylated proteome. [Zhang Y, et al. Nat Methods 2013;10(10):981-4]

    PubMed: 23955771
  • Tumor necrosis factor-like weak inducer of apoptosis and fibroblast growth factor-inducible 14 mediate cerebral ischemia-induced poly(ADP-ribose) polymerase-1 activation and neuronal death. [Hailea WB, et al. Neuroscience 2010;171(4):1256-64]

    PubMed: 20955770



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