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Iniparib (BSI-201)

BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor.

Catalog No.S1087
4.5 5 1 Reviews 1 Product Citations
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Iniparib (BSI-201) Chemical Structure
Molecular Weight: 292.03

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

Iniparib (BSI-201) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Inhibitor Library (96-well)

Product Information

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Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor.
Targets
IC50
In vitro 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
Clinical Trials
Features

Protocol(Only for Reference)

Cell Assay: [3]

Cell lines MDA-MB-231, and MDA-MB-436
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 5, and 9 days
Method 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.
1

References

Chemical Information

Download Iniparib (BSI-201) SDF
Molecular Weight (MW) 292.03
Formula

C7H5IN2O3
CAS No. 160003-66-7
Synonyms SAR240550
Solubility (25°C)
  • DMSO 58 mg/mL
  • Water <1 mg/mL
  • Ethanol 28 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name 4-iodo-3-nitrobenzamide
Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (1)


Click to enlarge 		Rating
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)

Product Citations (1)

  • 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), 1256-1264]

    PubMed: 20955770

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions
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