GSK467

GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members[1][2].

Product Specifications

CAS Number

[1628332-52-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk467.html

Concentration

10mM

Purity

99.55

Solubility

DMSO : 20.83 mg/mL (ultrasonic)

Smiles

O=C1C2=C(NC(OC3=CN(N=C3)CC4=CC=CC=C4)=N1)C=NC=C2

Molecular Formula

C17H13N5O2

Molecular Weight

319.32

Precautions

H302, H315, H319, H335

References & Citations

[1]Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12 (7) :539-45.|[2]Fu YD, et al. Targeting histone demethylase KDM5B for cancer treatment. Eur J Med Chem. 2020 Dec 15;208:112760.|[3]Guo JC, et al. KDM5B promotes self-renewal of hepatocellular carcinoma cells through the microRNA-448-mediated YTHDF3/ITGA6 axis. J Cell Mol Med. 2021 Apr 7;25 (13) :5949–62.