Germinone A 是一种新型强效 HTL/KAI2 激动剂，可刺激拟南芥种子萌发，在多种癌症中具有抗肿瘤活性。

Germinone A is a novel potent agonist of HTL/KAI2, stimulating activity for Arabidopsis seed germination, has antitumor activity in multiple types of carcinomas.

CRT0066101 suppressed the proliferation and migration of four bladder cancer cell lines in vitro.?CRT0066101 blocked tumor growth in a mouse flank xenograft model of bladder cancer.?To further assess the role of PKD in bladder carcinoma, examined the three PKD isoforms and found that PKD2 was highly expressed in eight bladder cancer cell lines and in urothelial carcinoma tissues from the TCGA database,?and that short hairpin RNA (shRNA)-mediated knockdown of PKD2 dramatically reduced bladder cancer growth and invasion in vitro and in vivo, suggesting that the effect of the compound in bladder cancer is mediated through inhibition of PKD2.?This notion was corroborated by demonstrating that the levels of phospho-PKD2 were markedly decreased in CRT0066101-treated bladder tumor explants.?CRT0066101 treatment or PKD2 silencing arrested bladder cancer cells at the G2/M phase, the arrest being accompanied by decreases in the levels of cyclin B1, CDK1 and phospho-CDK1 (Thr161) and increases in the levels of p27Kip1 and phospho-CDK1 (Thr14/Tyr15).?Moreover, CRT0066101 downregulated the expression of Cdc25C, which dephosphorylates/activates CDK1, but enhanced the activity of the checkpoint kinase Chk1, which inhibits CDK1 by phosphorylating/inactivating Cdc25C.?CRT0066101 was found to elevate the levels of Myt1, Wee1, phospho-Cdc25C (Ser216), Gadd45α, and 14-3-3 proteins, all of which reduce the CDK1-cyclin B1 complex activity.?CRT0066101 suppresses bladder cancer growth by inhibiting PKD2 through induction of G2/M cell cycle arrest, leading to the blockade of cell cycle progression[1].

T9007

C17H13NO5

311.29

3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years