中文名:RK-33
英文名:RK-33
英文别名:2H-Diimidazo[4,5-d:4',5'-f][1,3]diazepin-2-one, 3,7-dihydro-3,7-bis[(4-methoxyphenyl)methyl]-
纯度:10mM in DMSO
货号:R408134
包装:1ml
Cas号:1070773-09-9
存储温度:-80℃储存
产品介绍:
Information
RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
In vitro
RK-33 binds specifically to DDX3, but not to the closely related proteins DDX5 and DDX17. RK-33 inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. RK-33 has no effect on either mitochondrial respiration or ATP generation. RK-33 curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. RK-33 impairs radiation-induced DNA damage repair by inhibiting NHEJ activity.
In vivo
RK-33 in combination with radiation induces tumor regression in multiple mouse models of lung cancer. RK-33, at the dose used, is non-toxic in SCID mice. RK-33-treated mice do not exhibit any discernable morphological changes.
Cell Data
cell lines:
Concentrations:7.5 μM
Incubation Time:12 h
Powder Purity:≥99%
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关键字: 2H-?Diimidazo[4,?5-?d:4',?5'-?f]?[1,?3]?diazepin-?2-?one, 3,?7-?dihydro-?3,?7-?bis[(4-?methoxyphenyl)?methyl]?-
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