ML216, also known as CID-4985229, is a potent and selective inhibitor of Bloom (BLM) Helicase. ML216 displays low micromolar potency and selectivity over related helicases, such as RECQ1, RECQ5, and E. coli UvrD helicases. 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. ML216 shows strong selectivity for BLM in cultured cells. ML216 also inhibits cell proliferation of BLM-proficient fibroblast cells (PSNF5) while having only minimal effects on BLM-deficient fibroblast cells (PSNG13), indicating on-target activity in a cellular context.
CAS Number: 1430213-30-1
Molecular Weight: 383.32
Chemical Name: 1-[4-fluoro-3-(trifluoromethyl)phenyl]-3-[5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl]urea
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
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