NSC636819 is a cell permeable and selective novel active-site KDM4A/KDM4B inhibitor with IC50 ~6.4 μM for KDM4A and 9.3 μM for KDM4B. It inhibits histone demethylase activity on H3K9me3 and induces apoptosis in LNCaP prostate cancer cells in vitro. It also negatively regulates androgen-responsive genes. The overexpression of KDM4A/KDM4B in prostate cancer and their association with androgen receptor suggest that KDM4A/KDM4B are potential progression factors for prostate cancer.
CAS Number: 1618672-71-1
Molecular Weight: 510.15
Chemical Name: 4,4'-((1E,1'E)-(4,6-dinitro-1,3-phenylene)bis(ethene-2,1-diyl))bis(1,2-dichlorobenzene)
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 10 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
NSC636819 was used at 10 µM final concentration in vitro and in cellular assays.
- Chu CH, et al. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. (2014) J Med Chem. 57(14):5975-85.
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