Description
KDM5-C70 is an ethyl ester derivative of KDM5-C49, which is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability; therefore KDM5-C70 was developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use. KDM5-C70 increases H3K4me3 levels in myeloma cells. Treatment of MCF7 and MDA-MB-231 breast cancer cells with KDM5-C70 significantly increased global levels of H3K4me3 while having little impact on H3K4me2/me1 or modifications regulated by other histone lysine demethylases.
Product information
CAS Number: 1596348-32-1
Molecular Weight: 336.43
Formula: C17H28N4O3
Chemical Name: ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
Smiles: CN(C)CCN(CC)C(=O)CNCC1=CC(=CC=N1)C(=O)OCC
InChiKey: WCILOMUUNVPIKQ-UHFFFAOYSA-N
InChi: InChI=1S/C17H28N4O3/c1-5-21(10-9-20(3)4)16(22)13-18-12-15-11-14(7-8-19-15)17(23)24-6-2/h7-8,11,18H,5-6,9-10,12-13H2,1-4H3
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
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
How to use
In Vitro:
KDM5-C70 was used at 1-10 µM in vitro and cellular assays.
In Vivo:
possible use for in vivo study (IP dosing 15-50 mg/kg, bid)
References:
- Marc Labelle, et al. Inhibitors of Histone Demethylases. (2014). PCT WO 2014053491
- Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. (2016) Nat Chem Biol. 12(7):539-45.
- Horton JR, et al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. (2016) Cell Chem Biol. 23(7):769-81.
Products are for research use only. Not for human use.
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