JJ-450 是非竞争性拮抗剂,靶向雄激素受体 (AR),可以抑制野生型 AR 和 突变型 ARF876L 的转录活性。在 PC3 细胞中,JJ-450 抑制 AR 转录活性的 IC50 约为 1-10 μM,具有对 AR 的选择性结合特性,不与雄激素竞争 AR 的配体结合域 (LBD)。JJ-450 通过抑制 AR 的核转运并促使未结合配体的 AR 在细胞核内降解,影响 AR 及其剪切变体(如 ARF876L)的转录活性。该化合物可用于研究 Enzalutamide (MDV3100) 耐药的去势抵抗性前列腺癌 (CRPC)。
TSPA is an ATF6α translocation inducer which effectively promotes ATF6α translocation into the nucleus and ameliorates glucose homeostasis on db/db mice.
Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp . Luke ová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect
TTC-352 is an orally bioavailable selective human estrogen receptor alpha (ERalpha; ESR1; ERa) partial agonist (ShERPA), with potential antineoplastic activity. Upon administration, TTC-352 mimics the naturally-occurring 17beta-estradiol (E2) and targets and binds to ERa located in the nucleus. This causes translocation of ERa to extranuclear sites. Nuclear export of ERa prevents normal ER-mediated signaling and inhibits proliferation of ER-positive tumor cells.
MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA. The mechanism of causing unstable of HIF-1α mRNA by MPT0B098 is through decreasing RNA-binding protein, HuR, translocation from the nucleus to the cytoplasm. Notably, MPT0B098 effectively suppresses tumor growth and microvessel density of tumor specimens in vivo. Taken together, our results provide a novel mechanism of inhibiting HIF-1α of a microtubule inhibitor MPT0B098. MPT0B098 is......
NS-0011 is an inhibitor of CDK5 translocation which increases CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis.
Alisol B acetate can induce Bax nuclear translocation and apoptosis in human hormone-resistant prostate cancer PC-3 cells, the Bax activation and translocation from the cytosol to nucleus might be a crucial response to the apoptotic effect. Alisol B aceta