NCGC00244536 (Synonyms: KDM4B Inhibitor B3)

Name: NCGC00244536
Brand: MedChemExpress
SKU: HY-101799
Rating: 5.0 (1 reviews)

Cat. No.: HY-101799 Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

NCGC00244536 is a potent KDM4B inhibitor with an IC₅₀ of 10 nM.

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

NCGC00244536 Chemical Structure

CAS No. : 2003260-55-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 333	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 333	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 396	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2520	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE NCGC00244536

•Acta Pharmacol Sin. 2021 Apr 13. [Abstract]

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View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

NCGC00244536 is a potent KDM4B inhibitor with an IC₅₀ of 10 nM.

IC₅₀ & Target

KDM4

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	< 1 μM Compound: 72	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability by MTT assay	[PMID: 26710088]
PC-3	IC₅₀	40 nM Compound: 72	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay	[PMID: 26710088]
Sf9	IC₅₀	10 nM Compound: 72	Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using H3K4me3 as substrate Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using H3K4me3 as substrate	[PMID: 26710088]
VCaP	IC₅₀	< 1 μM Compound: 72	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability by MTT assay	[PMID: 26710088]

In Vitro

NCGC00244536 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^[1].

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

In Vivo

Treatment 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^[1].

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

Molecular Weight

382.45

Formula

C₂₅H₂₂N₂O₂

CAS No.

2003260-55-5

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(NCCCC1=CC=CC=C1)C2=CC=CC(C3=CC(O)=C4N=CC=CC4=C3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 36.67 mg/mL (95.88 mM; Need ultrasonic; 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	2.6147 mL	13.0736 mL	26.1472 mL
5 mM	0.5229 mL	2.6147 mL	5.2294 mL
10 mM	0.2615 mL	1.3074 mL	2.6147 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.75 mg/mL (7.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (245 KB) HNMR (289 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

Cell Assay ^[1]	LNCaP cells are treated with 0.1, 0.2, 1, 2.5, 5, 20 μM of NCGC00244536. Cell viability is measured using the MTT assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mouse: For xenograft animal model, PC3 cell suspension is injected into 4-6 weeks old severe combined immunodeficient (SCID) mice. When tumors become palpable, animals are randomly grouped for drug treatment. Alzet osmotic minipump containing NCGC00244536 (20 mg/kg)is subcutaneously inserted into each animal, which allowed continuous drug delivery to the tumor site for up to 5 days. Tumor volume is recorded every other days and calculated by using the ellipsoid formula^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6147 mL	13.0736 mL	26.1472 mL	65.3680 mL
	5 mM	0.5229 mL	2.6147 mL	5.2294 mL	13.0736 mL
	10 mM	0.2615 mL	1.3074 mL	2.6147 mL	6.5368 mL
	15 mM	0.1743 mL	0.8716 mL	1.7431 mL	4.3579 mL
	20 mM	0.1307 mL	0.6537 mL	1.3074 mL	3.2684 mL
	25 mM	0.1046 mL	0.5229 mL	1.0459 mL	2.6147 mL
	30 mM	0.0872 mL	0.4358 mL	0.8716 mL	2.1789 mL
	40 mM	0.0654 mL	0.3268 mL	0.6537 mL	1.6342 mL
	50 mM	0.0523 mL	0.2615 mL	0.5229 mL	1.3074 mL
	60 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0895 mL
	80 mM	0.0327 mL	0.1634 mL	0.3268 mL	0.8171 mL

NCGC00244536 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:

NCGC002445362003260-55-5KDM4B Inhibitor B3NCGC 00244536NCGC-00244536Histone DemethylaseInhibitorinhibitorinhibit

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NCGC00244536 (Synonyms: KDM4B Inhibitor B3)

Customer Review

NCGC00244536 Related Antibodies

1 Publications Citing Use of MCE NCGC00244536

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

NCGC00244536 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

NCGC00244536 Related Classifications

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