BG45

製品コードS7689 バッチS768901

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	C₁₁H₁₀N₄O
	分子量	214.22	CAS No.	926259-99-6
Solubility (25°C)*	体外	DMSO	42 mg/mL (196.06 mM)
		Ethanol	2 mg/mL warmed with 50ºC water bath (9.33 mM)
		Water	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	BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively.
in vitro	BG45 causes significant cell growth inhibition and induces caspase-dependent apoptosis in a series of MM cells. In RPMI8226 cells, BG45 synergistically enhances bortezomib-induced cytotoxicity. ^[1]
in vivo	In mice bearing MM.1S xenograft of human MM, BG45 (50 mg/kg, i.p.) significantly inhibits MM tumor growth. When in combination with bortezomib, BG45 (50 mg/kg, i.p.) enhances bortezomib-induced cytotoxicity. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MM.1S, RPMI8226, U266, H929, MM.1 R, RPMI-LR5, OPM1, OPM2 and RPMI-DOX40 cells
	濃度	~30 μM
	反応時間	48 h
	実験の流れ	The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [³H]thymidine uptake.
動物実験	動物モデル	Mice bearing MM.1S xenograft
	投薬量	50 mg/kg, 5 days a week
	投与方法	i.p.

参考

[1] Minami J, et al. Leukemia. 2014, 28(3), 680-689.

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：

HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364]	PubMed: 38284882
Selective Targeting of Class I HDAC Reduces Microglial Inflammation in the Entorhinal Cortex of Young APP/PS1 Mice [ Int J Mol Sci, 2023, 24(5)4805]	PubMed: 36902234
A Class I HDAC Inhibitor BG45 Alleviates Cognitive Impairment through the CaMKII/ITPKA/Ca2+ Signaling Pathway [ Pharmaceuticals (Basel), 2022, 15(12)1481]	PubMed: 36558932
HDAC8 cooperates with SMAD3/4 complex to suppress SIRT7 and promote cell survival and migration. [ Nucleic Acids Res, 2020, 6;48(6):2912-2923]	PubMed: 31970414
Class I HDAC Inhibitor Improves Synaptic Proteins and Repairs Cytoskeleton Through Regulating Synapse-Related Genes In vitro and In vivo [ Front Aging Neurosci, 2020, 12:619866]	PubMed: 33542682
Histone deacetylase inhibitor BG45-mediated HO-1 expression induces apoptosis of multiple myeloma cells by the JAK2/STAT3 pathway [ Anticancer Drugs, 2018, 29(1):61-74]	PubMed: 29049036

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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