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454862 Sigma-Aldrich

MNK1/2 Inhibitor II, ETP-45835 - Calbiochem

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: 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, MNK1/2 Inhibitor II, ETP-45835 - Calbiochem

  • Empirical Formula (Hill Notation) C13H16N4 · 2HCl

  • Molecular Weight 301.21

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, L to O,
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  desiccated
  protect from light
storage conditions   -20C
color   white
solubility   water: 50 mg/mL
shipped in   ambient

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

10 mg in Glass bottle

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.

Safety & Documentation

Safety Information

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