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ML216 Sale

(Synonyms: N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲,CID-49852229) 目录号 : GC12786

An inhibitor of the DNA repair enzyme Bloom helicase

ML216 Chemical Structure

Cas No.:1430213-30-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥546.00
现货
5mg
¥431.00
现货
10mg
¥714.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

IC50: 3.0 and 0.97 μM for full length BLM and BLM636–1298, respectively

ML216 is a potent inhibitor of the DNA unwinding activity of BLM helicase.

BLM helicase is reported to be a DNA unwinding enzyme critical in DNA repair through the homologous recombination pathway. BLM gene mutations lead to diminished BLM helicase activity and can cause Bloom’s Syndrome. Similar to other DNA repair enzymes, BLM helicase inhibition shows sensitization of tumor cells to conventional cancer therapies, such as camptothecin.

In vitro: ML216 showed submicromolar potency and selectivity over related helicases including RECQ1, RECQ5, and E. coli UvrD helicases. ML216 also inhibited cell proliferation of BLM-proficient fibroblast cells while had minimal effects on BLM deficient fibroblast cells, indicating on-target activity in a cellular context. Additionally, ML216 increased the frequency of sister chromatid exchanges, which was a diagnostic cellular phenotype consistent with the absence of a functional BLM protein [1].

In vivo: ML216 was a suitable starting point for further mouse tumor xenograft models and for the further development of potential cancer therapeutics [1].

Clinical trial: N/A

Reference:
[1] Rosenthal AS,Dexheimer TS,Nguyen G,Gileadi O,Vindigni A,Simeonov A,Jadhav A,Hickson I,Maloney DJ.  Discovery of ML216, a Small Molecule Inhibitor of Bloom (BLM) Helicase. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2011 Apr 15

Chemical Properties

Cas No. 1430213-30-1 SDF
别名 N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲,CID-49852229
化学名 1-(4-fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
Canonical SMILES FC(C(C(F)(F)F)=C1)=CC=C1NC(NC2=NN=C(C3=CC=NC=C3)S2)=O
分子式 C15H9F4N5OS 分子量 383.32
溶解度 ≥ 10.65mg/mL in DMSO with gentle warming 储存条件 Desiccate at -20°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6088 mL 13.0439 mL 26.0879 mL
5 mM 0.5218 mL 2.6088 mL 5.2176 mL
10 mM 0.2609 mL 1.3044 mL 2.6088 mL
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