CPI-455 HCl

製品コードS8287 バッチS828701

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₁₅ClN₄O
	分子量	314.77	CAS No.	2095432-28-1
Solubility (25°C)*	体外	DMSO	Insoluble
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	CPI-455 HClは特異的なKDM5阻害剤であり、標準的な化学療法または標的薬剤で処理された複数の癌細胞株モデルにおいて、H3K4トリメチル化（H3K4me3）の全体レベルを上昇させ、DTPの数を減少させました。
in vitro	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.

製品説明

CPI-455 HClは特異的なKDM5阻害剤であり、標準的な化学療法または標的薬剤で処理された複数の癌細胞株モデルにおいて、H3K4トリメチル化（H3K4me3）の全体レベルを上昇させ、DTPの数を減少させました。

in vitro

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.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines
	濃度	0-25 μM
	反応時間	14-20 days
	実験の流れ	All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×10⁵ cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain.

参考

https://pubmed.ncbi.nlm.nih.gov/27214401/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inhibition of fatty acid oxidation enables heart regeneration in adult mice [ Nature, 2023, 622(7983):619-626]	PubMed: 37758950
Methionine restriction promotes cGAS activation and chromatin untethering through demethylation to enhance antitumor immunity [ Cancer Cell, 2023, 41(6):1118-1133.e12]	PubMed: 37267951
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602]	PubMed: 37148583
Epigenetically suppressed tumor cell intrinsic STING promotes tumor immune escape [ Biomed Pharmacother, 2023, 157:114033]	PubMed: 36436495
Immune suppressive signaling regulated by latent transforming growth factor beta binding protein 1 promotes metastasis in cervical cancer [ Braz J Med Biol Res, 2023, 55:e12206]	PubMed: 36629522
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7]	PubMed: 35332332
Inhibition of KDM5A attenuates cisplatin-induced hearing loss via regulation of the MAPK/AKT pathway [ Cell Mol Life Sci, 2022, 79(12):596]	PubMed: 36396833
METTL3 promotes intrahepatic cholangiocarcinoma progression by regulating IFIT2 expression in an m6A-YTHDF2-dependent manner [ Oncogene, 2022, 10.1038/s41388-022-02185-1]	PubMed: 35094011
Demethylation at enhancer upregulates MCM2 and NUP37 expression predicting poor survival in hepatocellular carcinoma patients [ J Transl Med, 2022, 20(1):49]	PubMed: 35093119
pncCCND1_B Engages an Inhibitory Protein Network to Downregulate CCND1 Expression upon DNA Damage [ Cancers (Basel), 2022, 14(6)1537]	PubMed: 35326688

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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