551590

Quercetagetin

A cell-permeable flavanol compound that acts a potent, ATP-competitive, and reversible inhibitor of PIM1 kinase (IC₅₀ = 340 nM).

• Synonym(s): Quercetagetin, 3,3ʹ,4ʹ,5,6,7-Hexahydroxyflavone
• Empirical Formula (Hill Notation): C₁₅H₁₀O₈
• CAS Number: 90-18-6
• Molecular Weight: 318.24
• 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: yellow to yellow-green
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C15H10O8/c16-6-2-1-5(3-7(6)17)15-14(22)13(21)10-9(23-15)4-8(18)11(19)12(10)20/h1-4,16-20,22H
• InChI key: ZVOLCUVKHLEPEV-UHFFFAOYSA-N

Description

General description

A cell-permeable flavanol compound that acts a potent, ATP-competitive, and reversible inhibitor of PIM1 kinase (IC₅₀ = 340 nM). Exhibits ≥7-fold selectivity over 8 other kinases tested, including PIM2 (IC₅₀ = 3.45 µM), and little activity toward c-Abl even at concentrations as high as 200 µM. Inhibits cellular BAD phosphorylation (IC₅₀ = 5.5 µM) and induces growth arrest (ED₅₀ = 3.8 µM) in PIM1-expressing RWPE2 cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PIM1 kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 340 nM against PIM1 kinase

Packaging

Packaged under inert gas

Warning

Toxicity: Toxic & Carcinogenic / Teratogenic (G)

Reconstitution

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

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Holder, S., et al. 2007. Mol. Cancer Ther.6, 163.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable