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Key Documents

512533

Sigma-Aldrich

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(e):

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

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About This Item

Empirische Formel (Hill-System):
C16H11N3
Molekulargewicht:
245.28
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
protect from light

Farbe

yellow

Löslichkeit

DMSO: 100 mg/mL

Versandbedingung

ambient

Lagertemp.

2-8°C

Allgemeine Beschreibung

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 (Ki = 3.36 µM), and MT-noncompetitive (Ki = 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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Regulatory Review (Z)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Federico Gulluni et al.
Science (New York, N.Y.), 374(6573), eabk0410-eabk0410 (2021-12-10)
Cytokinetic membrane abscission is a spatially and temporally regulated process that requires ESCRT (endosomal sorting complexes required for transport)–dependent control of membrane remodeling at the midbody, a subcellular organelle that defines the cleavage site. Alteration of ESCRT function can lead
Onur Sen et al.
Developmental cell, 56(22), 3082-3099 (2021-11-11)
Chromosome mis-segregation during mitosis leads to aneuploidy, which is a hallmark of cancer and linked to cancer genome evolution. Errors can manifest as "lagging chromosomes" in anaphase, although their mechanistic origins and likelihood of correction are incompletely understood. Here, we

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