ML216 是一种选择性、细胞渗透性的BLM解旋酶抑制剂，具有抗肿瘤活性。它对BLMfull-length和BLM636-1298的IC50分别为 2.98 μM 和 0.97 μM。

ML-216 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).

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].

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].

1430213-30-1

C15H9F4N5OS

383.32

CID-49852229

DMSO:5 mg/mL (13 mM)),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years