1. Epigenetics
  2. Histone Demethylase
  3. NCGC00244536

NCGC00244536 (Synonyms: KDM4B Inhibitor B3)

Cat. No.: HY-101799 Purity: 98.02%
Handling Instructions

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

NCGC00244536 Chemical Structure

CAS No. : 2003260-55-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 333 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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

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Description

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

IC50 & Target

IC50: 10 nM (KDM4B)[1]

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].

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].

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

Molecular Weight

382.45

Formula

C₂₅H₂₂N₂O₂

CAS No.
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 : 36.67 mg/mL (95.88 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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
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Product Name:
NCGC00244536
Cat. No.:
HY-101799
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