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  3. NSC 617145

NSC 617145 

Cat. No.: HY-110185
Handling Instructions

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.

For research use only. We do not sell to patients.

NSC 617145 Chemical Structure

NSC 617145 Chemical Structure

CAS No. : 203115-63-3

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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].

MCE 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.
Molecular Weight

400.04

Formula

C₁₃H₁₀Cl₄N₂O₄

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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NSC 617145
Cat. No.:
HY-110185
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