JQKD82 dihydrochloride

• CAT Number: I047698
• CAS Number: 2863635-05-4
• Molecular Formula: C27H40N4O5.2HCl
• Molecular Weight: 573.55
• Purity: ≥95%
• IUPAC Name: [2,4-di(propan-2-yloxy)phenyl] 2-[[[2-[2-(dimethylamino)ethyl-ethylamino]-2-oxoethyl]amino]methyl]pyridine-4-carboxylate
• InChI: InChI=1S/C27H40N4O5/c1-8-31(14-13-30(6)7)26(32)18-28-17-22-15-21(11-12-29-22)27(33)36-24-10-9-23(34-19(2)3)16-25(24)35-20(4)5/h9-12,15-16,19-20,28H,8,13-14,17-18H2,1-7H3
• SMILES: CCN(CCN(C)C)C(=O)CNCC1=NC=CC(=C1)C(=O)OC2=C(C=C(C=C2)OC(C)C)OC(C)C

JQKD82 dihydrochloride is a cell-permeable and selective KDM5 inhibitor which increases histone H3K4me3 but paradoxically inhibits downstream MYC-driven transcriptional output in vitro and in vivo. JQKD82 is a prodrug-type KDM5 inhibitor which delivers the active binding molecule KDM5-C49 to potently block KDM5 function in multiple myeloma cells both in vitro and in vivo (IC50 value of 0.42 μM in MM.1S cells).
KEYWORDS: JQKD82 dihydrochloride | Supplier | KDM5 inhibitor | JQKD 82 | JQKD-82 | CAS [2863635-05-4] | [2410512-38-6] | [2863676-87-1] | Histone | Histone demethylase | Inhibitor | Enzymes | Lysine Demethylase 5A | Multiple myeloma | H3K4me3

Reference

H Ohguchi et al. Lysine Demethylase 5A is Required for MYC Driven Transcription in Multiple Myeloma. Blood Cancer Discov. 2021 Jul;2(4):370-387.