生物活性 | |||
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描述 | ATPase family AAA domain-containing protein 5 (ATAD5) is a tumor suppressor responsible for the maintenance of genomic stability and the inhibition of tumorigenesis. ML367 is a probe molecular that inhibits ATAD5 stabilization with an IC50 value of 1.2μM. In cells deficient in DNA damage repair proteins, such as PARP1, Lig3, Lig4, FancM, FancG, and Rad54b, treatment with ML367 significantly inhibited cell growth in colony formation assays. In HEK293T cells transfected with FLAG-tagged ATAD5, treatment with 20 μM 5-FUrd resulted in an increase in ATAD5 expression as compared to DMSO-treated controls, whereas ML367 at the concentrations of 5 – 40μM inhibited the elevated protein expression of ATAD5 in 5-FUrd-treated cells. The microsomal stability (T1/2) of ML367 in rats is 11min. The stability of ML367 to human liver microsomes is 57.9% after 30min. The mouse plasma stability (T1/2) of ML367 is >90min. | ||
作用机制 | ML367 is an inhibitor of ATAD5 stabilization that blocks UV irradiation-induced DNA damage responses, including CHK1-phosphorylation and RPA32-phosphorylation. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.99mL 0.60mL 0.30mL |
14.96mL 2.99mL 1.50mL |
29.91mL 5.98mL 2.99mL |