OTSSP167

Protein target name:

MELK

Mechanism of action:

Inhibitor, ATP competitive

Recommended Concentration for use in cells:

up to 100 nM

Probe Availability

MedChemExpress

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

CAMK

HUGO ID:

HGNC:16870

Entrez gene ID:

9833

UNIPROT ID:

Q14680

Target alias:

HPK38

Probe Details

Chemical Probes Portal ID:

CPP123

Probe alias:

AMX10201, OST167, OT5

PubChem CID:

71543332

ChEMBL ID:

CHEMBL3688339

SMILES string:

CC(=O)C1=CN=C2C=CC(=C3C=C(C(=O)C(=C3)Cl)Cl)NC2=C1NC4CCC(CC4)CN(C)C

InChi Key:

WZJUACDPTWDYSI-UHFFFAOYSA-N

Control compound:

Cpd1

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

0.41 nM

Potency assay:

In vitro kinase assay using recombinant proteins

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

4CQG

In cell validation

On target activity in cells

Potency in cells:

IC50

6.7, 4.3, 2.3, 6.0 and 97 nM

Target engagement assay (cells):

Cell Proliferation inhibition (A549 6.7 nM, T47D 4.3nM, DU4475 2.3nM, 22Rv1 6.0 nM, HT1197 97 nM)

In vivo validation

Organism:

Mouse

Dose:

1-20 mg/Kg

Route of delivery:

OralIntravenous

Primary Reference

Reference (doi):

10.18632/oncotarget.790

Reference (PMID):

23283305

Under Review

This probe is in the process of SAB review. Please continue to check back for new reviews and commentary.

SAB Rating

Rating for use in Cells

2 review(s)

Rating for use in Model Organisms

2 review(s)

SAB Members

SAB 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).

Jun 12 2016 - 2:48pm

Broad kinase selectivity data is not available for this compound.

Jun 12 2016 - 2:48pm

Sep 10 2021 - 11:11am

OTSSP167

Probe Availability

Probe Information

Target Details

HPK38

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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OTSSP167

Probe Availability

Probe Information

Target Details

HPK38

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?