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Sigma-Aldrich

KDM4A/KDM4B Inhibitor, NSC636819

Sinónimos:

KDM4A/KDM4B Inhibitor, NSC636819, JMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor

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About This Item

Fórmula empírica (notación de Hill):
C22H12Cl4N2O4
Número de CAS:
Peso molecular:
510.15
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥97% (HPLC)

Quality Level

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.
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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
KDM4A/B
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Chia-Han Chu et al.
Journal of medicinal chemistry, 57(14), 5975-5985 (2014-06-28)
The KDM4/JMJD2 Jumonji C-containing histone lysine demethylases (KDM4A-KDM4D), which selectively remove the methyl group(s) from tri/dimethylated lysine 9/36 of H3, modulate transcriptional activation and genome stability. The overexpression of KDM4A/KDM4B in prostate cancer and their association with androgen receptor suggest

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