666-15 是一种有效的选择性 CREB 抑制剂，IC₅₀ 为 81 nM。666-15 抑制乳腺癌异种移植模型中的肿瘤生长。

666-15 is a potent and selective CREB inhibitor with an IC 50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

Solid

IC50: 81 nM (CREB)

666-15 (73 nM; for 12 hours) significantly blocks the effects caused by MSN overexpression, including cell proliferation, invasion, soft agar colony formation ability, and the expression of CREB downstream genes. 666-15 inhibits MSN overexpression-induced CREB phosphorylation.
666-15 (1μM; pretreated 2 hour) effectively inhibits PE-induced CREB phosphorylation. 666-15 significantly decreases the protein expression of ANP and β-MHC and inhibits the activation of ER stress, including the expression of GRP78, CHOP, ATF6, and the phosphorylation of IRE1 in PE?+?siRNA?+?666-15 group and PE?+?si-CTRP3?+?666-15 group.
666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and 0.31 μM.

666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J Med Chem. 2015 Jun 25;58(12):5075-87.
[2]. Qin Y, et al. Interfering MSN-NONO complex-activated CREB signaling serves as a therapeutic strategy for triple-negative breast cancer. Sci Adv. 2020 Feb 19;6(8):eaaw9960.

In Vitro: DMSO : 125 mg/mL (201.44 mM; ultrasonic and warming and heat to 60°C)配制储备液