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.

• Synonym(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
• Empirical Formula (Hill Notation): C₂₃H₂₆IN₇O₂S
• CAS Number: 702675-74-9
• Molecular Weight: 591.47
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale yellow
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 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)
• InChI key: VAVXGGRQQJZYBL-UHFFFAOYSA-N

Description

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable