MKI-3

MKI-3 : Inhibitor of MASTL

Structure

SERP Rating

Probe MKI-3 is in the process of SERP review.

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Information

MASTL

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q96GX5

Target Class: Kinase

Target SubClass: AGC

Potency: IC50

Potency Value: 5.72 ± 0.18 nM

Potency Assay: Biochemical assay (HTRF Assay)

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

Target aliases:

Serine/threonine-protein kinase greatwall, THC2, M ...

DOI Reference: 10.1021/acs.jmedchem.5c03599

Uniprot ID: Q96GX5

Target Class: Kinase

Target SubClass: AGC

Potency: Kd

Potency Value: 1.89 nM

Potency Assay: SPR

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

Target aliases:

Serine/threonine-protein kinase greatwall, THC2, M ...

DOI Reference: 10.1021/acs.jmedchem.5c03599

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): MKI-3 selectively inhibited MASTL over other AGC kinases, including large tumor suppressor kinase 1 (LATS1), LATS2, 70-kDa ribosomal protein S6 kinase, phosphoinositide-dependent protein kinase 1, protein kinase A, protein kinase C alpha, and Rho-associated coiled-coil containing protein kinase 1

Potency assay (off target): To further assess the kinase selectivity of MKI-3, we screened 82 kinases, including those with high sequence or structural similarity to MASTL.

Probe Selectivity in Vitro:

Among the kinases tested, only five out of 82 exhibited over 80% inhibition, indicating a favorable selectivity profile and minimal off-target activity.

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SERP ratings and comments

No SERP comments found for MKI-3