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ML216

Chemical Structure : ML216

CAS No.: 1430213-30-1

ML216 (ML 216;ML-216;CID49852229)

Catalog No.: PC-42991Not For Human Use, Lab Use Only.

ML216 (CID49852229) is a potent, selective inhibitor of DNA unwinding activity of BLM (Bloom's syndrome protein) with IC50 of 2.98 and 0.97 uM for full length BLM and BLM636-1298, respectively.

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Biological Activity

ML216 (CID49852229) is a potent, selective inhibitor of DNA unwinding activity of BLM (Bloom's syndrome protein) with IC50 of 2.98 and 0.97 uM for full length BLM and BLM636-1298, respectively.
ML216 weak inhibits WRN helicase (IC50=12.6 uM) and does not inhibit RecQ1, RecQ5 and UrvD (IC50>50 uM).
ML216 disrupts BLM’s binding to DNA, rather than being an inhibitor of ATP binding by BLM, the inhibition of ssDNA-dependent ATPase activity with Ki of 1.76 uM,.
ML216 shows cell-based activity and can induce sister chromatid exchanges, enhances the toxicity of aphidicolin, and exerts antiproliferative activity in cells expressing BLM.

Physicochemical Properties

M.Wt 383.3235
Formula C15H9F4N5OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 1.71 mg/mL

Chemical Name/SMILES

Urea, N-[4-fluoro-3-(trifluoromethyl)phenyl]-N'-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]-

References

1. Nguyen GH, et al. Chem Biol. 2013 Jan 24;20(1):55-62.

2. Rosenthal AS, et al. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5660-6.

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