1. Epigenetics
  2. Histone Demethylase
  3. NCGC00244536

NCGC00244536 (Synonyms: KDM4B Inhibitor B3)

Cat. No.: HY-101799 Purity: 98.57%
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
10 mM * 1 mL in DMSO USD 333 In-stock
Estimated Time of Arrival: December 31
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
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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].

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].

Molecular Weight

382.45

Formula

C₂₅H₂₂N₂O₂

CAS No.

2003260-55-5

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (261.47 mM)

*"≥" means soluble, but saturation unknown.

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.
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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