NSC 617145

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NSC 617145  纯度: 98.68%

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

NSC 617145 Chemical Structure

CAS No. : 203115-63-3

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
50 mg ￥2800 In-stock
100 mg ￥4500 In-stock
200 mg   询价  
500 mg   询价  

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NSC 617145 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

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].

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

400.04

Formula

C13H10Cl4N2O4
CAS 号

203115-63-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (41.67 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4998 mL 12.4987 mL 24.9975 mL
5 mM 0.4999 mL 2.4997 mL 4.9995 mL
10 mM 0.2500 mL 1.2499 mL 2.4997 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (4.17 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (4.17 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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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