The first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1

ML-216 – 10 mg

Brand:
Cayman
CAS:
1430213-30-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}  

 

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Description

The first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM); 25-50 μM dose-dependently inhibits the proliferation of BLM-expressing PSNF5 fibroblast cells

Formal name: N-[4-fluoro-3-(trifluoromethyl)phenyl]-N’-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]-urea

Synonyms:  CID-49852229

Molecular weight: 383.3

CAS: 1430213-30-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|DNA Damage and Repair

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