Description
JQKD82, also known as PCK82, is a cell-permeable and selective KDM5 inhibitor (MM.1S cells, IC50 = 0.42 uM). JQKD82 increases histone H3K4me3 but paradoxically inhibits downstream MYC-driven transcriptional output in vitro and in vivo. JQKD82 is a useful tool compound to block KDM5A function as a potential therapeutic strategy for MM. QKD82 is a more stable ester of KDM5-C49 that is able to deliver the active molecule KDM5-C49 to cells more efficiently
Product information
CAS Number: 2410512-38-6
Molecular Weight: 610.01
Formula: C27H43Cl3N4O5
Chemical Name: 2, 4-diisopropoxyphenyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate trihydrochloride
Smiles: Cl.Cl.Cl.CN(C)CCN(CC)C(=O)CNCC1=CC(=CC=N1)C(=O)OC1=CC=C(C=C1OC(C)C)OC(C)C
InChiKey: VSTHCFWHQMJPDZ-UHFFFAOYSA-N
InChi: InChI=1S/C27H40N4O5.3ClH/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;3*1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Lysine Demethylase 5A is Required for MYC Driven Transcription in Multiple Myeloma Hiroto Ohguchi1*#, Paul M.C. Park2*, Tingjian Wang2*, Berkley E. Gryder3,4*, Daisuke Ogiya5, Keiji Kurata5, Xiaofeng Zhang2, Deyao Li2, Chengkui Pei2, Takeshi Masuda6, Catrine Johansson7, Virangika K. Wimalasena2, Yong Kim3, Shinjiro Hino8, Shingo Usuki9, Yawara Kawano10, Mehmet K. Samur5, Yu-Tzu Tai5, Nikhil C. Munshi5, Masao Matsuoka10, Sumio Ohtsuki6, Mitsuyoshi Nakao8, Takashi Minami11, Shannon Lauberth12, Javed Khan3, Udo Oppermann7,13, Adam D. Durbin14, Kenneth C. Anderson5,15#, Teru Hideshima5#, Jun Qi2,15,16#
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