A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom's syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97uM, 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 without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 > 1.2h) and plasma stability (~100% at 5h).
Storage and Stability:Store at -20°C under inert atmosphere. Protect from light. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
