| Name | NCGC00244536 |
|---|---|
| Synonyms |
NC00244536,inhibit,Histone Demethylase,NC00244536,Inhibitor,NC-00244536
KDM4B Inhibitor B3 KDM4B INHIBITOR COMPOUND B3 NC00244536 ,E0132 NC00244536, 10 mM in DMSO 3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide NC00244536(Benzamide) KDM4B-IN-B3 Benzamide, 3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl) NC00244536 |
| Description | NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM. |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C25H22N2O2 |
|---|---|
| Molecular Weight | 382.45 |
| Storage condition | 2-8℃ |