OTSSP167

OTSSP167: ATP competitive inhibitor of MELK

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe OTSSP167 is in the process of SERP review.

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Information

MELK

Inhibitor, ATP competitive

DOI - 10.18632/oncotarget.790

Probe Availability:

In Vitro Validations

Uniprot ID: Q14680

Target Class: Protein kinase

Target SubClass: CAMK

Potency: IC50

Potency Value: 0.41 nM

Potency Assay: In vitro kinase assay using recombinant proteins

PDB ID for probe-target interaction (3D structure): 4CQG

Target aliases:

Maternal embryonic leucine zipper kinase, KIAA0175 ...

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Broad kinase selectivity data is not available for this compound.

(last updated: 6 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Recently reported selectivity data show that this is not a selective MELK inhibitor (http://www.kinase-screen.mrc.ac.uk/screening-compounds/594372). Based on the selectivity data, I do not recommend this compound as a probe to use in cells or model organisms even though this molecule has entered into Phase 1 clinical trials. OTSSP167 abrogates mitotic checkpoint through inhibiting multiple mitotic kinases (http://dx.doi.org/10.1371/journal.pone.0153518).

(last updated: 16 May 2016 )