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ML216

CAS No. : 1430213-30-1

MCE 站：ML216

产品活性：ML216 (CID-49852229) 是一种有效，选择性，细胞渗透性的 BLM 解旋酶抑制剂，对 BLM^full-length 和 BLM^636-1298 的 IC₅₀ 分别为 2.98 μM 和 0.97 μM。ML216 以 K_i 为 1.76 µM 来抑制 BLM 的 ssDNA 依赖性 ATPase 的活性。ML216 具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：DNA/RNA Synthesis

In Vitro: ML216 (12.5-50 µM; 24-72 hours; PSNG5 ａnd PSNG13cells) treatment inhibits the proliferation of PSNF5 cells in a concentration-dependent manner, but not of PSNG13 cells.
ML216 treatment leads to a statistically significant increase in the frequency of sister chromatid exchanges (SCEs) in PSNF5 cells, but not in PSNG13 cells.
ML216 increases the sensitivity of PSNF5 cells to aphidicolin but has no sensitizing effect on isogenic PSNG13 cells devoid of BLM.
ML216 inhibits both the full length WRN (IC₅₀ of 5 μM) ａnd a truncated WRN^500-946 (IC₅₀ of 12.6 μM), with the former being 2.5-fold more sensitive to inhibition. BLM is a little more sensitive than WRN to inhibition by ML216 (1.7-fold based on IC₅₀ values). Despite the detectable inhibition of WRN by ML216, this compound appears selective for BLM in human cells. ML216 inhibits proliferation of WRN⁺ ａnd WRN⁻ cells equally well, ａnd similarly sensitized both cell types to aphidicolin.

In Vivo: Although ML216 inhibits unwinding by the sequence-related BLM ａnd WRN helicases similarly in vitro, the apparent dependence on BLM for ML216 to exert its biological effects in human cells suggests BLM specificity for the drug’s mechanism of action in vivo. A co-crystal structure of BLM in complex with inhibitor would be informative. Cellular cues in vivo may induce a specific conformation of WRN that makes it resistant to ML216.

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