Sigma-Aldrich Creb Inhibitor 666-15

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
desiccated (hygroscopic)
protect from light

Color

off-white

Solubility

DMSO: 100 mg/mL

Storage Temp.

−20°C

General Description

A cell-permeable naphthol derivative that acts as a highly potent and selective inhibitor of cAMP response element-binding protein (CREB)-mediated gene transcription (IC50 = 81 nM by CREB RLuc reporter assay with transfected HEK 293T cells). Also shown to inhibit forskolin-stimulated transcription of Nurr1/NR4A2 (~ 50 nM). Diminishes CREB phosphorylation and reduces colony forming ability of wild-type AML cells. Inhibits the growth of cancer cells (GI₅₀= 46, 73, 310 and 470 nM for MDA-MB-468, MDA-MB-231, MCF-7, and A549, respectively) without affecting normal cells. Completely suppresses the growth of MDA-MB-468 xenografts in mice (~ 10 mg/kg, i.p., 5 days/week for 5 weeks).A cell-permeable naphthol derivative that acts as a highly potent and selective inhibitor of cAMP response element-binding protein (CREB)-mediated gene transcription (IC50 = 81 nM by CREB RLuc reporter assay with transfected HEK 293T cells). Also shown to inhibit forskolin-stimulated transcription of Nurr1/NR4A2 (~ 50 nM). Diminishes CREB phosphorylation and reduces colony forming ability of wild-type AML cells. Inhibits the growth of cancer cells (GI₅₀= 46, 73, 310 and 470 nM for MDA-MB-468, MDA-MB-231, MCF-7, and A549, respectively) without affecting normal cells. Completely suppresses the growth of MDA-MB-468 xenografts in mice (~ 10 mg/kg, i.p., 5 days/week for 5 weeks).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
CREBReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical Form

Supplied as HCl salt

Other Notes

Kang, X., et Al. 2015.Nat. Cell. Biol. 17,665.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany