NSC 617145

Research use only, not for human use.

NSC 617145 is a novel small-molecule, selective inhibitor of WRN helicase with IC50 of 230 nM.

NSC 617145 is a novel small-molecule, selective inhibitor of WRN helicase with IC50 of 230 nM; shows no significant inhibition on BLM, FANCJ, ChlR1, RecQ, and UvrD; acts synergistically with very low concentrations of mitomycin C to inhibit proliferation in a WRN-dependent manner and induce DSB and chromosomal abnormalities in FA-D2(-/-) cells.

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.NSC 617145 (0.75 μM; 6 hours) induces WRN binding to chromatin and proteasomal degradation.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.NSC 617145, induces cell cycle arrest and apoptosis in human T-cell leukemia virus type 1 (HTLV-1)-transformed adult T-cell leukemia cells. Cell Viability Assay 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 Cell Line:HeLa cells Concentration:0.75 μM Incubation Time:6 hours Result:Caused WRN to become degraded by a proteasome-mediated pathway.

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NSC617145

Cell Cycle/DNA Damage

DNA Repair Protein

DNA Repair Protein

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203115-63-3

400.04

C13H10Cl4N2O4

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (25.00 mM)

CC(C)(CN1C(=O)C(=C(C1=O)Cl)Cl)CN2C(=O)C(=C(C2=O)Cl)Cl

1,1'-(2,2-Dimethyl-1,3-propanediyl)bis[3,4-dichloro-1H-pyrrole-2,5-dione

(-20℃)

With Ice Pack

≥ 2 years