NSC636819, KDM4A/KDM4B Inhibitor

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.

Product information

CAS Number: 1618672-71-1

Molecular Weight: 510.15

Formula: C22H12Cl4N2O4

Chemical Name: 4,4'-((1E,1'E)-(4,6-dinitro-1,3-phenylene)bis(ethene-2,1-diyl))bis(1,2-dichlorobenzene)

Smiles: [O-][N+](=O)C1C=C(C(=CC=1/C=C/C1=CC(Cl)=C(Cl)C=C1)/C=C/C1=CC(Cl)=C(Cl)C=C1)[N+]([O-])=O

InChiKey: YYZPXBXVBQSBDG-IJIVKGSJSA-N

InChi: InChI=1S/C22H12Cl4N2O4/c23-17-7-3-13(9-19(17)25)1-5-15-11-16(22(28(31)32)12-21(15)27(29)30)6-2-14-4-8-18(24)20(26)10-14/h1-12H/b5-1+,6-2+

Technical Data

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: ≥360 days 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:

NSC636819 was used at 10 µM final concentration in vitro and in cellular assays.

References:

1. 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.

Products are for research use only. Not for human use.