CPI-455 HCl |
| カタログ番号GC25305 |
CPI-455 HClは、酵素アッセイにおけるフルレングスKDM5Aの半数阻害濃度（IC50）が10±1 nMであり、H3K4トリメチル化（H3K4me3）のグローバルレベルを上昇させ、標準化学療法またはターゲット治療薬で処理された多くのがん細胞株モデルにおいてDTPsの数を減少させます。この製品は溶解性が低く、動物実験は可能ですが、細胞実験については注意して選択してください！
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2095432-28-1
Sample solution is provided at 25 µL, 10mM.
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CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
CPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site[1].
[1] Vinogradova M, et al. Nat Chem Biol. 2016, 12(7):531-8.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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