NCGC00244536

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NCGC00244536
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Cat #: V3301 CAS #: 2003260-55-5 Purity ≥ 98%

Description: NCGC00244536 (also known as KDM4B Inhibitor B3; KDM4B-IN-B3) is a novel and potent inhibitor of the Histone lysine demethylase KDM4 with an IC50 of 10 nM.

References: Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96.

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Product Promise

Promise
Molecular Weight (MW)382.46
Molecular FormulaC25H22N2O2
CAS No.2003260-55-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥100mg/mLr
Water: N/Ar
Ethanol: N/A
SMILES CodeO=C(NCCCC1=CC=CC=C1)C2=CC=CC(C3=CC(O)=C4N=CC=CC4=C3)=C2
SynonymsKDM4B-IN-B3; KDM4B IN B3; KDM4BINB3; KDM4B Inhibitor B3; KDM4B Inhibitor-B3; KDM4B Inhibitor B-3
ProtocolIn VitroNCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC50=40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC50s.
In VivoTreatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.6147 mL13.0733 mL26.1465 mL52.2931 mL
5mM0.5229 mL2.6147 mL5.2293 mL10.4586 mL
10mM0.2615 mL1.3073 mL2.6147 mL5.2293 mL
20mM0.1307 mL0.6537 mL1.3073 mL2.6147 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.