5.38341

666-15

≥98% (HPLC), solid, CREB inhibitor, Calbiochem^®

• Synonyma: CREB Inhibitor, 666-15, 3-(3-Aminopropoxy)-N-(2-((3-((4-chloro-2-hydroxyphenyl)carbamoyl)naphthalen-2-yl)oxy)ethyl)-2-naphthamide, HCl, CBP-CREB Interaction Inhibitor II, 666-15
• Empirický vzorec (Hillův zápis): C₃₃H₃₀ClN₃O₅ · xHCl
• Molekulová hmotnost: 584.06 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Vlastnosti

• Název produktu: CREB Inhibitor, 666-15,
• assay: ≥98% (HPLC)
• 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
• Quality Level: 100

Popis

Biochem/physiol Actions

Primary Target
CREB

Reversible: yes

Cell permeable: yes

Disclaimer

Toxicity: Standard Handling (A)

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).

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.

Other Notes

Kang, X., et al. 2015. Nat. Cell. Biol.17, 665.

Packaging

Packaged under inert gas

Physical form

Supplied as HCl salt

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable