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Description

A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom&prime,s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97 microM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (>Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 >1.2 h) and plasma stability (~100% at 5 h).