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NCGC00244536

Catalog No. TQ0050 CAS 2003260-55-5

Synonyms: KDM4B Inhibitor B3

NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

NCGC00244536, CAS 2003260-55-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 327.00
10 mg	In stock	$ 497.00
25 mg	In stock	$ 793.00
50 mg	In stock	$ 1,130.00
100 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 273.00

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Purity: 99.72%

Purity: 99.15%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM).
Targets&IC50	KDM4B:10 nM
In vitro	NCGC00244536 significantly suppresses the growth of AR-positive cell lines such as LNCaP and VCaP, demonstrating inhibitory concentration values (IC50s) below one micromolar, while effectively eliminating androgen-induced LNCaP cell proliferation. It exhibits strong preference for rapidly proliferating AR-negative PC3 cells with a strikingly low IC50 of 40 nM, demonstrating greater than 100-fold selectivity compared to immortalized prostate epithelial cell lines PrEC1 and PrEC4. Additionally, NCGC00244536 effectively restricts the expansion of various other cancer cell lines, including breast cancer cell lines MDA-MB2 and MCF-7, showcasing its inhibitory potential across a broad spectrum of cancer types with IC50s in the micromolar range.
In vivo	Treatment with NCGC00244536 significantly inhibits tumor growth without causing major toxicity in animals, which appear normal. Tumors treated with NCGC00244536 show a substantial increase in cell apoptosis, necrosis, and fibrosis.
Cell Research	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.
Animal Research	For the 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.

Synonyms	KDM4B Inhibitor B3
Molecular Weight	382.45
Formula	C25H22N2O2
CAS No.	2003260-55-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (261.47 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library NO PAINS Compound Library Methylation Compound Library Epigenetics Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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You can also refer to dose conversion for different animals. More

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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:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NCGC00244536 2003260-55-5 Chromatin/Epigenetic Histone Demethylase inhibit NCGC-00244536 KDM4B Inhibitor B3 Inhibitor NCGC 00244536 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.