NSC 617145 是一种选择性 werner 综合征解旋酶 (WRN) 解旋酶抑制剂，IC₅₀ 值为 230 nM。NSC 617145 抑制 WRN ATPase，并诱导双链断裂 (DSB) 和染色体异常。NSC 617145 对 WRN 具有选择性，优于 BLM、FANCJ、ChlR1、RecQ 和 UvrD 解旋酶。

NSC 617145 is a selective werner syndrome helicase (WRN) helicase inhibitor with an IC 50 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.

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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.

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[1]. Monika Aggarwal, et al. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway. Cancer Res. 2013 Sep 1;73(17):5497-507.
[2]. R Moles, et al. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells. J Hematol Oncol. 2016 Nov 9;9(1):121.

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