204001

BX-795

BX-795, also referenced under CAS 702675-74-9, modulates the biological activity of multiple kinases. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : BX-795, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I, N-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase, N-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I, Aurora Kinase Inhibitor VIII
• Formule empirique (notation de Hill): C₂₃H₂₆IN₇O₂S
• Numéro CAS: 702675-74-9
• Poids moléculaire : 591.47
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: pale yellow
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)
• Clé InChI: VAVXGGRQQJZYBL-UHFFFAOYSA-N

Description

Description générale

A cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC₅₀ = 11 nM for PDK1 at ≤ 10 µM of ATP; IC₅₀ = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC₅₀ = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer³⁹⁶), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Clark, K., et al. 2009. J. Biol. Chem.284, 14136.
Tamgumcy, T., et al. 2008. Exp. Cell Res.314, 2299.
Feldman, R.I., et al. 2005. J. Biol. Chem.280, 19867.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable