| Name | NCGC00244536 |
| Description | NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM). |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (261.47 mM)
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| Keywords | inhibit | NCGC-00244536 | Histone Demethylase | Inhibitor | NCGC00244536 | NCGC 00244536 |
| Inhibitors Related | LSD1-IN-24 | Tranylcypromine hemisulfate | DDP-38003 dihydrochloride | GSK-LSD1 dihydrochloride | GSK-J4 | FY-21 | Daminozide | Zavondemstat | AS8351 | Procaine hydrochloride | JIB-04 | KDM4-IN-4 |
| Related Compound Libraries | Methylation Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
