NSC 617145 |
| رقم الكتالوجGC18507 |
NSC 617145 هو مثبط هليكاز متلازمة ويرنر الانتقائي (WRN) مع قيمة IC50 تبلغ 230 نانومتريثبط NSC 617145 WRN ATPase ، ويؤدي إلى حدوث فواصل مزدوجة (DSB) وتشوهات الكروموسوماتيظهر NSC 617145 انتقائيًا لـ WRN عبر طائرات BLM و FANCJ و ChlR1 و RecQ و UvrD
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Cas No.: 203115-63-3
Sample solution is provided at 25 µL, 10mM.
NSC 617145 is targeted inhibitor of werner syndrome helicase (WRN) helicase, with an IC50 value of 230nM [1]. NSC 617145 can induce synthetic lethality via a genetic-based and/or chemically induced mechanism and render human cells deficient in the Fanconi Anemia (FA) pathway hypersensitive to the DNA cross-linking agent mitomycin C (MMC) in a WRN-dependent manner[2]. NSC 617145 has been widely used as an anti-cancer agent and has been applied in various cancer cell models to induce DNA damage[3].
In vitro, NSC 617145 treatment for 48 hours significantly inhibited the proliferation of PC3 cells, K562 cells, and HeLa cells, with IC50 values of 184.6 ± 36.3, 20.3 ± 11.5, and 237.0 ± 120.2nM, respectively[4]. Treatment with 250nM NSC 617145 for 4 days significantly reduced the number of LMY1 cells and induced cell apoptosis[5]. NSC 617145 treatment for 48 hours exhibited significant cytotoxicity in normal human liver LX2 cells and normal human renal epithelial HK2 cells, with the IC50 values of 1.81 ± 0.27μM and 5.64 ± 0.96μM, respectively[6].
References:
[1] Aggarwal M, Banerjee T, Sommers J A, et al. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway[J]. Cancer research, 2013, 73(17): 5497-5507.
[2] Datta A, Brosh Jr R M. New insights into DNA helicases as druggable targets for cancer therapy[J]. Frontiers in molecular biosciences, 2018, 5: 59.
[3] Aggarwal M, Banerjee T, Sommers J A, et al. Targeting an Achilles’ heel of cancer with a WRN helicase inhibitor[J]. Cell cycle, 2013, 12(20): 3329-3335.
[4] Li H, Yu J, Yu G, et al. Design and synthesis of N-aryl-2-trifluoromethyl-quinazoline-4-amine derivatives as potential Werner-dependent antiproliferative agents[J]. Molecular Diversity, 2025, 29(1): 195-214.
[5] Moles R, Bai X T, Chaib-Mezrag H, et al. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells[J]. Journal of hematology & oncology, 2016, 9(1): 121.
[6] Yu J, Yu G, Cheng S, et al. Quinazoline Derivative kzl052 Suppresses Prostate Cancer by Targeting WRN Helicase to Stabilize DNA Replication Forks[J]. International Journal of Molecular Sciences, 2025, 26(13): 6093.
| Cell experiment [1]: | |
Cell lines | LMY1 cells |
Preparation Method | LMY1 cells were cultured in RPMI-1640 medium supplemented with penicillin, streptomycin and 10% fetal bovine serum (FBS). The cells were treated with NSC 617145 (0.02, 0.2, 2, and 20μM) or DMSO as a control. After 96 hours, the inhibition of cell growth was measured by cell counting. |
Reaction Conditions | 0.02, 0.2, 2, and 20μM; 96h |
Applications | NSC 617145 treatment significantly inhibited the cell proliferation of LMY1 cells. |
References: | |
| Cas No. | 203115-63-3 | SDF | |
| Chemical Name | 1,1'-(2,2-dimethyl-1,3-propanediyl)bis[3,4-dichloro-1H-pyrrole-2,5-dione | ||
| Canonical SMILES | CC(CN(C(C(Cl)=C1Cl)=O)C1=O)(C)CN2C(C(Cl)=C(Cl)C2=O)=O | ||
| Formula | C13H10Cl4N2O4 | M.Wt | 400 |
| الذوبان | 1mg/mL in DMSO, 2mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5 mL | 12.5 mL | 25 mL |
| 5 mM | 500 μL | 2.5 mL | 5 mL |
| 10 mM | 250 μL | 1.25 mL | 2.5 mL |
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