LH168

LH168 : Inhibitor of WDR5

Structure

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In Cells

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Probe LH168 is in the process of SERP review.

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Information

WDR5

Inhibitor

Up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P61964

Target Class: WD repeat

Target SubClass: WD40 repeat

Potency: Kd

Potency Value: 13 nM

Potency Assay: SPR

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

Target aliases:

WD repeat-containing protein 5, BIG3, WDR5, WDR5_H ...

Other Reference: Peer reviewed at SGC

Uniprot ID: P61964

Target Class: WD repeat

Target SubClass: WD40 repeat

Potency: Kd

Potency Value: 38 nM

Potency Assay: ITC

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

Target aliases:

WD repeat-containing protein 5, BIG3, WDR5, WDR5_H ...

Other Reference: Peer reviewed at SGC

Uniprot ID: P61964

Target Class: WD repeat

Target SubClass: WD40 repeat

Potency: ΔTm

Potency Value: 19.8 K

Potency Assay: DSF

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

Target aliases:

WD repeat-containing protein 5, BIG3, WDR5, WDR5_H ...

Other Reference: Peer reviewed at SGC

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): LH168 was tested against 13 histone/arginine methyltransferases by radioactivity-based assay, none of them was significantly inhibited by LH168 at 50 μM. In addition, WDR5 and 7 arginine binders were evaluated in DSF assay using LH168 at 50 μM concentration. As a result, only WDR5 showed significant Tm shift.

Potency assay, off target (cells): Proteomic analysis of a sample enriched by pull down experiment A cell lysate was subjected to pull down using streptavidin beads and biotinylated analogue of chemical probe. Subsequent proteomic analysis revealed that the samples was enriched for WDR5 as expected. To confirm the selectivity, the pull down experiment was repeated, this time with the co-treatment with excess of LH168 chemical probe which selectively outcompetes the binding to LH205 and therefore prevents the pull down of WDR5 using streptavidin beads.

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(last updated: 7 Feb 2025 )