454862

MNK1/2 Inhibitor II, ETP-45835

The MNK1/2 Inhibitor II, ETP-45835 controls the biological activity of MNK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): MNK1/2 Inhibitor II, ETP-45835, 4-(3-(Piperidin-4-yl)-1H-pyrazol-5-yl)pyridine, diHCl, ETP45835, MNK Inhibitor II, Mitogen-Activated Protein Kinase-Interacting Kinase Inhibitor II, ETP45835, MNK Inhibitor II, Mitogen-Activated Protein Kinase-Interacting Kinase Inhibitor II, 4-(3-(Piperidin-4-yl)-1H-pyrazol-5-yl)pyridine, diHCl
• Empirical Formula (Hill Notation): C₁₃H₁₆N₄ · 2HCl
• CAS Number: 2136571-30-5
• Molecular Weight: 301.21
• MDL number: MFCD27919983
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 50 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: C1(C2=CC=NC=C2)=CC(C3CCNCC3)=NN1

Description

General description

A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC₅₀ = 646 and 575 nM, respectively, against MNK1 and MNK2) with much reduced or little activity against 24 other kinases (≤15% inhibition at 5 µM). Reported to exhibit good aqueous solubility (>100 µM at pH 7.4) and inhibit the proliferation (IC₅₀ = 17 µM) and cellular eIF4E Ser²⁰⁹ phosphorylation (IC₅₀ = 4.7 µM) of MV4:11 cells.

A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC₅₀ = 646 and 575 nM, respectively, against MNK1 and MNK2) with much reduced or little activity against a panel of 24 other kinases (≤15% inhibition at 5 µM), including MNK upstream kinases B-Raf, ERK1, MEK1, and p38α. Reported to exhibit good aqueous solubility (>100 µM at pH 7.4) and inhibit the proliferation (IC₅₀ = 17 µM) and cellular eIF4E Ser²⁰⁹ phosphorylation (IC₅₀ = 4.7 µM) of acute myeloid leukemia MV4:11 cells.

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

Oyarzabal, J., et al. 2010. J. Med. Chem.53, 6618.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable