QC6352 | Inhibitor of KDM4C
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDM4C
  • IC50:35 ± 8 nM
  • EC50:3.5 ± 1 nM
  • EC50:1.3 ± 0.3 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - KDM4B 56 ± 6 nM, KDM4D 104 ± 18 nM, KDM4A 104 ± 10nM

Selectivity Assessment Description:
Enzymatic activity (IC50 nM) KDM2B >4,000; KDM4C 35 ± 8; KDM3A >4,000; KDM4D 104 ± 18; KDM3B >4,00 ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
IMR-90 EC50 >30 uM

Potency
Cellular
In Vitro

KDM4C

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acsmedchemlett.7b00220

In Vivo Validations

Mouse
Dose: 5 , 10, 25, 50 mg/Kg
Route of delivery: Intravenous, Oral
Systemic clearance: 6.9 mL/min/kg (IV)

DOI Reference: 10.1021/acsmedchemlett.7b00220

Chemical Information

Molecular Formula C24H25N3O2
SMILEs CN(c1ccccc1)c1ccc2c(c1)CCC[C@H]2CNc1cnccc1C(=O)O
InChI InChI=1S/C24H25N3O2/c1-27(19-8-3-2-4-9-19)20-10-11-21-17(14-20)6-5-7-18(21)15-26-23-16-25-13-12-22(23)24(28)29/h2-4,8-14,16,18,26H,5-7,15H2,1H3,(H,28,29)/t18-/m0/s1
Molecular weight 387.19 Da
AlogP 5.079700000000004
HBond acceptors 5
HBond donors 2
Atoms 54

Vendors

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Expert Reviews


(on 14 Dec 2020)
Cellular Use Rating
In Model Organisms
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...
(on 14 Dec 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
(on 18 Dec 2020)
Cellular Use Rating
In Model Organisms
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...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria