CREB inhibitor (666-15)

Product NameCREB inhibitor (666-15)
CAS1433286-70-4
MFC33H31Cl2N3O5
MW620.53
EINECS
MOL File1433286-70-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMF: 5mg/mL; DMSO: 5mg/mL
form	A solid
color	White to off-white
Stability	Hygroscopic

Usage And Synthesis

Uses

3-(3-Aminopropoxy)-N-[2-[[3-[[(4-chloro-2-hydroxyphenyl)amino]carbonyl]-2-naphthalenyl]oxy]ethyl]-2-naphthalenecarboxamide Hydrochloride has been identified as an antitumor agent.

Biological Activity

CREB inhibitor (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription with IC50 of 81 nM. It also inhibits the growth of cancer cells without affecting normal cells.

in vitro

666-15 can effectively inhibit the growth of cancer cells. In MDA-MB-231 and MDA-MB-468 cells, the GI50 values of 666-15 were 73 nM and 46 nM, respectively. 666-15 also had strong activity in A549 and MCF-7 cells, with GI50 of 0.47 μM and 0.31 μM, respectively. 666-15 inhibits the transcriptional activity of CREB in live cells that do not depend on direct CREB or CBP binding reactions.

in vivo

In the in vivo MDA-MB-468 xenograft tumor model, 666-15 completely inhibited tumor growth without obvious toxicity. Intraperitoneal injection of 10 mg/kg of 666-15 in mice was well tolerated.

target