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NSC617145(WRN inhibitor)

  Cat. No.:  DC20228   Featured
Chemical Structure
203115-63-3
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Field of application
NSC617145 is a Werner syndrome helicase (WRN) helicase inhibitor (IC50 = 250 nM).
Cas No.: 203115-63-3
Chemical Name: NSC617145,NSC-617145,NSC 617145,WRN inhibitor
Synonyms: NSC617145,NSC-617145,NSC 617145,WRN inhibitor
SMILES: CC(CN1C(C(Cl)=C(Cl)C1=O)=O)(C)CN2C(C(Cl)=C(Cl)C2=O)=O
Formula: C13H10Cl4N2O4
M.Wt: 400.04
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: NSC 617145 is a selective werner syndrome helicase (WRN) helicase inhibitor with an IC50 value of 230 nM. NSC 617145 inhibits WRN ATPase, and induces double-strand breaks (DSB) and chromosomal abnormalities. NSC 617145 shows selective for WRN over BLM, FANCJ, ChlR1, RecQ, and UvrD helicases[1].
In Vitro: NSC 617145 (0.75-3 μM; 24-72 hours) shows maximal inhibition of proliferation (98%) at the lowest concentration in a WRN-specific manner in HeLa cells[1]. NSC 617145 (0.75 μM; 6 hours) induces WRN binding to chromatin and proteasomal degradation[1]. In FA-D2-/- cells, NSC 617145 (0.125 μM) acts synergistically with very low concentrations of Mitomycin C to inhibit proliferation in a WRN-dependent manner and induce double-strand breaks (DSB) and chromosomal abnormalities. NSC 617145 exposure results in enhanced accumulation of DNA-PKcs pS2056 foci and Rad51 foci in Mitomycin C-treated FA-deficient cells, suggesting that WRN helicase inhibition prevents processing of Rad51-mediated recombination products and activates NHEJ[1]. NSC 617145, induces cell cycle arrest and apoptosis in human T-cell leukemia virus type 1 (HTLV-1)-transformed adult T-cell leukemia cells[2]. Cell Viability Assay[1] Cell Line: HeLa cells Concentration: 0.75 μM, 1 μM, 1.5 μM, 2 μM, 3 μM Incubation Time: 24 hours, 48 hours, 72 hours Result: Inhibited cell proliferation in a WRN-specific manner. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0.75 μM Incubation Time: 6 hours Result: Caused WRN to become degraded by a proteasome-mediated pathway.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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