2. Epigenetics
  3. Histone Demethylase
  4. NSC636819

NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer.

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NSC636819

NSC636819 Estructura química

No. CAS : 1618672-71-1

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NSC636819 Related Antibodies

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Ver todos los productos específicos de isoformas Histone Demethylase:

Ver todas las isoformas
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Descripciòn

NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer[1][2].

IC50 & Target

KDM4

 

Cellular Effect
Cell Line Type Value Description References
LNCaP IC50
16.5 3
Compound: 4, NSC636819
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
[PMID: 24971742]
LNCaP IC50
16.5 3
Compound: 4, NSC636819
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
[PMID: 24971742]
LNCaP IC50
16.5 3
Compound: 4, NSC636819
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
[PMID: 24971742]
In Vitro

NSC636819 (compound 4) targets KDM4A and KDM4B with Ki of 5.5 μM and 3.0 μM, respectively[1].
NSC636819 (100 μM; 30 min) inhibits the demethylation activity of KDM4A and KDM4B and significantly reduces the level of H3K9me3 in LNCaP cells[1].
NSC636819 (5-20 μM; 3 d) is cytotoxic (LNCaP IC50 = 16.5 μM) and induces apoptosis in LNCaP cells[1].
NSC636819 (C-4) (10-20 μM; 2 d) strongly induces the expression of both TRAIL and its receptor DR5 selectively (mRNA and protein) in both TRAIL-sensitive (Calu-6 and MDA-MB231) and TRAIL-resistant cancer cells (A549 and H1299)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NSC636819 Related Antibodies

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 3 days
Result: Almost completely blocked the demethylating activity toward H3K9me3 at 5 μM.
Resulted the inhibition of KDM4A/KDM4B,that specifically inhibits the demethylating activity of H3K9me3 and strongly blocks cell growth.
In Vivo

NSC636819 (C-4) (20 or 40 mg/kg; ip; 5 times a week; 4 weeks) strongly suppresses A549 tumor growth and sensitizes tumors to TRAIL-inducer ONC201 in mouse model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A549 Lung cancer xenograft model in mice[2]
Dosage: 20 mg/kg, 40 mg/kg
Administration: ip; 5 times per weeks, 27 days; with or without ONC201 (i.p.; 25 mg/kg, 1 time a week).
Result: Dose-dependently inhibited the tumor growth, and sensitized tumors to TRAIL.
Induced tumor expression of TRAIL, DR5 and the level of cleaved caspase-7 and H3K9me3, whereas decreased the expression of KDM4A in xenograft tumors.
Peso molecular

510.15

Fòrmula

C22H12Cl4N2O4
No. CAS
Appearance

Solid

Color

Yellow to orange

SMILES

ClC1=C(Cl)C=CC(/C=C/C2=C([N+]([O-])=O)C=C([N+]([O-])=O)C(/C=C/C3=CC(Cl)=C(Cl)C=C3)=C2)=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 5.1015 mg/mL (10.00 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9602 mL 9.8010 mL 19.6021 mL
5 mM 0.3920 mL 1.9602 mL 3.9204 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 98.90%

SDS (251 KB)

COA (248 KB) Elemental Analysis Report (106 KB)

Instrucciones de manejo (2659 KB)
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9602 mL 9.8010 mL 19.6021 mL 49.0052 mL
5 mM 0.3920 mL 1.9602 mL 3.9204 mL 9.8010 mL
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NSC636819 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSC6368191618672-71-1NSC 636819NSC-636819Histone DemethylasecompetitiveselectiveKDM4A/KDM4Bprostate cancerInhibitorinhibitorinhibit

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Nombre del producto:
NSC636819
Cat. No.:
HY-110154
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