ML216
Based on 8 publication(s) in Google Scholar
ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLMfull-length and BLM636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 μM. Antitumor avtivity.
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- Pureza: 99.89%
- No. CAS: 1430213-30-1
- Fòrmula: C15H9F4N5OS
- Peso molecular:383.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML216
More- Nat Cancer. 2025 Feb;6(2):278-291. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1182-1193. [Abstract]
- J Transl Med. 2023 Jul 6;21(1):445. [Abstract]
- Cell Rep. 2025 May 10;44(5):115706. [Abstract]
- Cells. 2022 Dec 29;12(1):145. [Abstract]
- Int J Mol Sci. 2026 Apr 10;27(8):3425. [Abstract]
- Am J Cancer Res. 2021 Apr 15;11(4):1347-1368. [Abstract]
- Utrecht University. 2023 Feb.
Ver todos los productos específicos de isoformas DNA/RNA Synthesis
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Actividad biológica
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Helicase |
ML216 (12.5-50 μM; 24-72 hours; PSNG5 and PSNG13cells) treatment inhibits the proliferation of PSNF5 cells in a concentration-dependent manner, but not of PSNG13 cells[1].
ML216 treatment leads to a statistically significant increase in the frequency of sister chromatid exchanges (SCEs) in PSNF5 cells, but not in PSNG13 cells[1].
ML216 increases the sensitivity of PSNF5 cells to aphidicolin but has no sensitizing effect on isogenic PSNG13 cells devoid of BLM[1].
ML216 inhibits both the full length WRN (IC50 of 5 μM) and a truncated WRN500-946 (IC50 of 12.6 μM), with the former being 2.5-fold more sensitive to inhibition. BLM is a little more sensitive than WRN to inhibition by ML216 (1.7-fold based on IC50 values). Despite the detectable inhibition of WRN by ML216, this compound appears selective for BLM in human cells. ML216 inhibits proliferation of WRN+ and WRN cells equally well, and similarly sensitized both cell types to aphidicolin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PSNG5 and PSNG13cells
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Concentration:12.5 μM or 50 µM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Inhibited the proliferation of PSNF5 cells, but not of PSNG13 cells, and did so in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1430213-30-1
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Appearance Solid
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Peso molecular 383.32
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Fòrmula C15H9F4N5OS
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(F)C(C(F)(F)F)=C1)NC2=NN=C(S2)C3=CC=NC=C3
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Synonyms
CID-49852229
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Cancer
Targeting BRCA1-deficient PARP inhibitor-resistant cells with nickases reveals nick resection as a cancer vulnerability. [Abstract]2025 Feb;6(2):278-291. PMID: 39838098 -
Nat Chem Biol
2025 Aug;21(8):1182-1193. PMID: 39809895 -
J Transl Med
PARP1 negatively regulates transcription of BLM through its interaction with HSP90AB1 in prostate cancer. [Abstract]2023 Jul 6;21(1):445. PMID: 37415147 -
Cell Rep
Genomic context influences translesion synthesis DNA polymerase-dependent mechanisms of micronuclei induction by G-quadruplexes. [Abstract]2025 May 10;44(5):115706. PMID: 40349342 -
Cells
2022 Dec 29;12(1):145. PMID: 36611939 -
Int J Mol Sci
2026 Apr 10;27(8):3425. PMID: 42074068 -
Am J Cancer Res
BLM interaction with EZH2 regulates MDM2 expression and is a poor prognostic biomarker for prostate cancer. [Abstract]2021 Apr 15;11(4):1347-1368. PMID: 33948362 -
Solvente y solubilidad
DMSO : 20 mg/mL (52.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (5.22 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nguyen GH, et al. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells. Chem Biol. 2013 Jan 24;20(1):55-62. [Content Brief]
[2]. Banerjee T, et al. A new development in DNA repair modulation: discovery of a BLM helicase inhibitor. Cell Cycle. 2013 Mar 1;12(5):713-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6088 mL | 13.0439 mL | 26.0879 mL | 65.2197 mL |
| 5 mM | 0.5218 mL | 2.6088 mL | 5.2176 mL | 13.0439 mL | |
| 10 mM | 0.2609 mL | 1.3044 mL | 2.6088 mL | 6.5220 mL | |
| 15 mM | 0.1739 mL | 0.8696 mL | 1.7392 mL | 4.3480 mL | |
| 20 mM | 0.1304 mL | 0.6522 mL | 1.3044 mL | 3.2610 mL | |
| 25 mM | 0.1044 mL | 0.5218 mL | 1.0435 mL | 2.6088 mL | |
| 30 mM | 0.0870 mL | 0.4348 mL | 0.8696 mL | 2.1740 mL | |
| 40 mM | 0.0652 mL | 0.3261 mL | 0.6522 mL | 1.6305 mL | |
| 50 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3044 mL |
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