QC6352

Inhibitor of KDM4C

Structure

Information

Protein target names: KDM4C

Mechanism of action: Inhibitor

Recommended in-cell concentration:
up to 100 nM

In Vitro Validations

Uniprot ID: Q9H3R0
Target Class: Epigenetic
Target SubClass: Protein Demethylase
Potency: IC50
Potency Value: 35 ± 8 nM
Potency Assay: enzymatic screening assay (AlphaScreen and LANCE)
PDB ID for probe-target interaction (3D structure): 5VGI
Structure-activity relationship: yes
Target aliases:
Lysine-specific demethylase 4C, KIAA0780, JMJD2C, ...

DOI Reference: 10.1021/acsmedchemlett.7b00220

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

The compound represents an important advancement in the field, as it is a potent and selective probe molecule appropriate for both in vitro and in vivo work. Compound shows potent antiproliferative effects at 10 nM in BCS1 cells and even more robust effects at 50 nM in a 3D sphere forming assay.  Wonder if recommended dose in cells should be up to 50 nM instead of 100 nM, although given the selectivity profile 100 nM should be ok.

(last updated: 14 Dec 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 14 Dec 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

QC6352 is a chemical probe that inhibits KDM4 family members (KDM4A, KDM4B, KDM4C, and KDM4D) with good specificity within the Jumonji demethylase family. It has been characterised in cancer cell lines as well as organoids derived from breast and colon cancer patients for inhibition of growth. Finally, the drug has been shown to be effective at inhibiting tumour growth in xenograft mouse model of breast cancer through oral dosing. The compound is well tolerated by the mice at doses as high as 50 mg/kg for at least a month. However, no data was provided that showed that inhibition of the tumour growth in vivo was directly tied to the enzymatic activity of the KDM4 family members.

(last updated: 18 Dec 2020 )