JQKD82 dihydrochloride，5MG，SML4212-5MG，Sigma

General description

JQKD82 dihydrochloride is histone H3K4 demethylase inhibitor is a produg of KDM5-C49 phenol ester prodrug that selectively upregulates H3K4me3 and inhibits KDM5-dependent cancer growth.
(KDOAM-21; KDM5A/B/C/D Ki = 2/1/6.1/3.4 nM vs. KDM4C/6B/3A/2A Ki =0.51/4.55/2.59/4.4 μM; KDM5A/B/C/D IC50 = 1.1/0.8/3.2/2.7 μM by FDH assay with[αKG] = 1 mM & [E]/[S] = 0.5/15 μM; KDM5A/B/C IC50 = 25/30/59 nM by alphaLISA with [αKG] = 25 μM & [E]/[S] = 10/100 nM). JQKD82 selectively upregulates cellular histone H3K4me3 with a higher efficacy than KDM5-C49 orKDM5-C70 (3 μM for 24 h; MM.1S cells), and inhibits myeloma growth in cultures (MM.1S IC50 = 0.42 μM vs IC50 3.1 μM/KDM5-C70, >10 μM/KDM5-C49) and in vivo (50 mg/kg b.i.d. i.p. to mice with MOLP-8 xenograft).

Application

JQKD82 dihydrochloride may be used:

• to study its effects on lysine demethylase 5A (KDM5A) function in multiple myeloma research
• as a potential agent in HIV-1 research, where it was evaluated for its ability to reactivate latent HIV-1 inT cells
• to study its effects on cell cycle arrest and apoptosis induction

Biochem/physiol Actions

A selective and cell-permeable lysine demethylase 5(KDM5) inhibitor.

Disclaimer

Hygroscopic