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.

For research use only. We do not sell to patients.

NSC636819 Chemical Structure

NSC636819 Chemical Structure

CAS No. : 1618672-71-1

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

NSC636819 Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 μM
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.
Molecular Weight

510.15

Formula

C22H12Cl4N2O4
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 98.90%

SDS (251 KB)

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

Handling Instructions (2659 KB)
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NSC636819
Cat. No.:
HY-110154
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.