Ro-3306

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ro-3306 是一种有效的、选择性的 ATP 竞争性 CDK1 抑制剂，针对 CDK1/cyclin B1 的 Ki 为 35 nM，相对于 CDK2/cyclin E 的选择性为 10 倍，相对于 CDK4/cyclin D 的选择性超过 50 倍。

Ro-3306 is a potent, selective, ATP-competitive CDK1 inhibitor with Ki of 35 nM against CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and >50-fold relative to CDK4/cyclin D; also inhibits CDK1/cyclin A complexes with Ki of 110 nM, shows >15-fold selectivity against a diverse panel of 8 human kinases; reversibly arrests human cells at the G(2)/M border of the cell cycle and allows for effective cell synchronization in early mitosis; enhances p53-mediated Bax activation and mitochondrial apoptosis in AML.

RO-3306 is an ATP-competitive inhibitor, and inhibits CDK1/cyclin A complexes with Ki of 110 nM. RO-3306 blocks the cell cycle in the G2/M phase of human cancer cells. RO-3306 (4 μM) induces apoptosis in cancer cells. RO-3306 (5 μM) induces G2/M-phase cell cycle arrest and apoptosis of AML cells in a time-dependent manner. RO-3306 treatment significantly increases the percentage of Annexin V-positive cells in G1-phase cells without affecting the cell cycle distribution. RO-3306 enhances p53-mediated apoptosis. RO-3306 cooperates with Nutlin-3 in activating Bax and inducing mitochondrial apoptosis. RO-3306 (5 μM) downregulates antiapoptotic p21, Bcl-2 and survivin protein expression in AML. RO-3306 inhibits p53-induced p21 synthesis. RO-3306 does not inhibit RNA polymerase II CTD phosphorylation. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces the blastocyst formation in oocytes.

——

Ro3306

Angiogenesis

CDK

CDK1|ERK|PKA|PKCδ|SGK

Cancer

——

872573-93-8

351.4453

C18H13N3OS2

>98% (HPLC)

DMSO: ≥ 47 mg/mL

O=C1N=C(NCC2=CC=CS2)S/C1=C/C3=CC=C4N=CC=CC4=C3

4(5H)-Thiazolone, 5-(6-quinolinylmethylene)-2-[(2-thienylmethyl)amino]-, (5Z)-

(-20℃)

With Ice Pack

≥ 2 years