IACS-52825

IACS-52825 : Inhibitor of MAP3K12

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe IACS-52825 is in the process of SERP review.

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Information

MAP3K12

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q12852

Target Class: Kinase

Target SubClass: STE

Potency: Kd

Potency Value: 1.3 nM

Potency Assay: Biochemical assay (KINOMEscan KdELECT)

PDB ID for probe-target interaction (3D structure): 8OUT

Target aliases:

Mitogen-activated protein kinase kinase kinase 12, ...

DOI Reference: 10.1021/acs.jmedchem.3c00788

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): CEREP PanLabs (10 μM) 0/80 Kinase screening (DiscoverX KINOMEscan, <35% control at 1 μM) 7/403

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a potent, highly optimized probe with good in vivo pharmacokinetic properties. A small number of off-target kinases are also inhibited at relevant concentrations, and this activity should be considered for phenotypic readouts.

(last updated: 2 Nov 2023 )