5.31996
KDM4A/KDM4B Inhibitor, NSC636819
Synonym(s):
KDM4A/KDM4B Inhibitor, NSC636819, JMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C22H12Cl4N2O4
CAS Number:
Molecular Weight:
510.15
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
solid
potency
3.0 μM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
brown
solubility
DMSO: 10 mg/mL
storage temp.
2-8°C
General description
A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC50 = 6.4 µM; Ki = 5.5 µM) and KDM4B (IC50 = 9.3 µM; Ki = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC50 = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
KDM4A/B
KDM4A/B
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chu, C.H., et al. 2014. Journ. Med. Chem.57, 5975.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5319960001 | 04055977287134 |