KLHL12-In-7k

KLHL12-In-7k : Inhibitor of KLHL12

Structure

SERP Rating

Probe KLHL12-In-7k is in the process of SERP review.

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Information

KLHL12

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q53G59

Target Class: E3 ubiquitin ligase adaptor / scaffold protein

Target SubClass: Kelch-like family

Potency: Ki

Potency Value: 330 nM

Potency Assay: FPA competition assay

PDB ID for probe-target interaction (3D structure): 9Y8K

Target aliases:

Kelch-like protein 12, C3IP1, KLHL12, KLH12_HUMAN, ...

DOI Reference: 10.1021/acs.jmedchem.5c02931

Uniprot ID: Q53G59

Target Class: E3 ubiquitin ligase adaptor / scaffold protein

Target SubClass: Kelch-like family

Potency: Kd

Potency Value: 480 nM

Potency Assay: SPR

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

Target aliases:

Kelch-like protein 12, C3IP1, KLHL12, KLH12_HUMAN, ...

DOI Reference: 10.1021/acs.jmedchem.5c02931

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity was assessed computationally and based on sequence similarities within the family.

Probe Selectivity in Vitro:

Ten of KLHL family proteins share sequence identity above 35% and are thus considered highly homologous with KLHL12. Analysing the Alpphafold structures of these homologs against the KLHL12-7k complex shows that KLHL1 and KLHL5 have a loop preventing binding. KLHL8, KLHL18, and KLHL19 (KEAP1) have the highest binding pocket similarity (>50%) therefore most likely to be off-targets.

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SERP ratings and comments

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