Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
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1 mg | 在庫あり | ¥ 22,500 | |||
5 mg | 在庫あり | ¥ 75,000 | |||
10 mg | 在庫あり | ¥ 114,000 | |||
25 mg | 在庫あり | ¥ 182,000 | |||
50 mg | 在庫あり | ¥ 259,500 | |||
100 mg | 在庫あり | ¥ 349,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 63,000 |
説明 | NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM). |
ターゲット&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. |
細胞研究 | 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. |
動物実験 | 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. |
別名 | KDM4B Inhibitor B3 |
分子量 | 382.45 |
分子式 | C25H22N2O2 |
CAS No. | 2003260-55-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (261.47 mM)
You can also refer to dose conversion for different animals. 詳細
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NCGC00244536 2003260-55-5 Chromatin/Epigenetic Histone Demethylase inhibit NCGC-00244536 KDM4B Inhibitor B3 Inhibitor NCGC 00244536 inhibitor