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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C16H11N3
Molecular Weight:
245.28
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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 (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.

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Regulatory Review (Z)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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