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ML216

Catalog No. T5413 CAS 1430213-30-1

Synonyms: CID-49852229

ML216 (CID-49852229) is a small molecule inhibitor of BLM helicase (IC50: 1.8 μM). It showed 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s < 50 μM).

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ML216, CAS 1430213-30-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 57.00
10 mg	In stock	$ 86.00
25 mg	In stock	$ 136.00
50 mg	In stock	$ 191.00
100 mg	In stock	$ 274.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 96.83%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ML216 (CID-49852229) is a small molecule inhibitor of BLM helicase (IC50: 1.8 μM). It showed 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s > 50 μM).
Targets&IC50	BLM:1.8 μM
In vitro	ML216 shows cell-based activity and can induce sister chromatid exchanges, enhance the toxicity of aphidicolin, and exert antiproliferative activity in cells expressing BLM, but not those lacking BLM [2].
Cell Research	Cells were treated with BLM inhibitors at the indicated concentrations for up to 72 hr. At each time point, the WST-1 reagent (a pale tetrazolium derivative converted to an intensely-colored formazan product by the action of mitochondrial dehydrogenases) was added, and after a 4 hr incubation the plates were analyzed optically at 450 nm with a reference wavelength of 690 nm [2].

Synonyms	CID-49852229
Molecular Weight	383.32
Formula	C15H9F4N5OS
CAS No.	1430213-30-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (13 mM), Sonification and heating are recommended.

References and Literature

1. Rosenthal AS, et al. Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5660-6. 2. 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.

Citations

1. Ma X Y, Xu H Q, Zhao J F, et al.Discovery of a Novel Bloom’s Syndrome Protein (BLM) Inhibitor Suppressing Growth and Metastasis of Prostate Cancer.International journal of molecular sciences.2022, 23(23): 14798. 2. Ma X Y, Zhao J F, Ruan Y, et al.ML216-Induced BLM Helicase Inhibition Sensitizes PCa Cells to the DNA-Crosslinking Agent Cisplatin.Molecules.2022, 27(24): 8790.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library DNA Damage & Repair Compound Library Cell Cycle Compound Library Anti-Infection Compound Library Anti-Aging Compound Library Covalent Inhibitor Library Anti-Cancer Compound Library Anti-Bacterial Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ML216 1430213-30-1 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis helicase ML 216 WRN DNA sister inhibit Anticancer CID-49852229 anti-proliferative CID 49852229 Inhibitor CID49852229 chromatid BLM unwinding toxicity ML-216 inhibitor

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