512533

MKLP-2 Inhibitor, Paprotrain

The MKLP-2 Inhibitor, Paprotrain controls the biological activity of MKLP-2. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonym(s): MKLP-2 Inhibitor, Paprotrain, (Z)-2-(1H-Indol-3-yl)-3-(pyridin-3-yl)acrylonitrile, PAssenger PROteins TRAnsport INhibitor, Mitotic Kinesin-Like Protein 2 Inhibitor
• Empirical Formula (Hill Notation): C₁₆H₁₁N₃
• Molecular Weight: 245.28
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable acrylonitrile compound that inhibits the kinesin-6 family member MKLP-2 (Mitotic kinesin-like protein 2; IC₅₀ against basal and microtubule-/MT-stimulated ATPase activity = 1.35 and 0.83 µM, respectively) in a reversible, ATP-uncompetitive (K_i = 3.36 µM), and MT-noncompetitive (K_i = 1.6 µM) manner, with little effect against the ATPase activity of 12 other kinesins (≤20% inhibition at 50 µM), including the close related MKLP-1 and MPP1 (M-phase phosphoprotein 1). Shown to inhibit cellular Aurora B and Survivin anaphase centromere-to-spindle midzone relocation in HeLa cultures (50 µM for 8 h), but not MKLP-1- or Kif4-mediated PRC1 relocation, resulting in misaligned chromosomes (70% of total metaphase cells), multipolar spindles (14% of total metaphase cells), and eventual apoptosis.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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

Other Notes

Tcherniuk, S., et al. 2010. Angew. Chem. Int. Ed.49, 8228.

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