GI254023X

製品コードS8660 バッチS866004

化学情報

	Synonyms	GI 4023, SRI028594	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₁H₃₃N₃O₄
	分子量	391.50	CAS No.	260264-93-5
Solubility (25°C)*	体外	DMSO	78 mg/mL (199.23 mM)
		Ethanol	78 mg/mL (199.23 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	GI254023X (GI 4023, SRI028594) is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively. GI254023X can inhibit MMP9.
in vitro	In cell-based cleavage experiments GI254023X potently blocks the constitutive release of IL6R, CX3CL1 and CXCL16, which is in line with the reported involvement of ADAM10 but not ADAM17 in this process. By contrast, the compound does not affect the PMA-induced shedding^[2]. In addition to ADAM10 and ADAM17, GI254023X is a moderate inhibitor of ADAM9 with an IC50 of 280 nM^[1].
in vivo	Acute treatment with GI254023X in an AD mouse model substantially reduces brain LRP1 shedding and increases Aβ40 levels in the plasma, indicating enhanced Aβ transit from the brain to the periphery. Furthermore, both soluble and insoluble Aβ40 and Aβ42 brain levels are decreased following GI254023X treatment, but these effects lack statistical significance^[5].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCA-7 cells
	濃度	3 μM
	反応時間	24 h
	実験の流れ	HCA-7 cells are treated for 24 h with 0.1% DMSO, the metalloprotease inhibitors GI (GI254023X, ADAM10-selective, 3 µM) and GW (GW280264X, ADAM10- and ADAM17-selective, 3 µM), the pan-metalloprotease inhibitor Marimastat (MM; 10 µM), and the EGF-R kinase inhibitor AG1478 (10 µM). Cells stimulated with 100 ng/ml EGF served as positive control. Tyrosine-phosphorylated EGF-R and total EGF-R are assessed by Western blot analysis.
動物実験	動物モデル	BALB/c mice
	投薬量	200 mg/kg
	投与方法	i.p.

参考

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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：

MAP4K4 promotes ovarian cancer metastasis through diminishing ADAM10-dependent N-cadherin cleavage [ Oncogene, 2023, 42(18):1438-1452]	PubMed: 36922678
Elevated Kir2.1/nuclear N2ICD defines a highly malignant subtype of non-WNT/SHH medulloblastomas [ Signal Transduct Target Ther, 2022, 7(1):72]	PubMed: 35273141
IDO1 can impair NK cells function against non-small cell lung cancer by downregulation of NKG2D Ligand via ADAM10 [ Pharmacol Res, 2022, 177:106132]	PubMed: 35183714
Fewer LAG-3+ T Cells in Relapsing-Remitting Multiple Sclerosis and Type 1 Diabetes [ J Immunol, 2022, 208(3):594-602]	PubMed: 35022272
Pore-forming alpha-hemolysin efficiently improves the immunogenicity and protective efficacy of protein antigens [ PLoS Pathog, 2021, 17(7):e1009752]	PubMed: 34288976
Staphylococcus aureus α-Toxin Induces Acid Sphingomyelinase Release From a Human Endothelial Cell Line [ Front Microbiol, 2021, 12:694489]	PubMed: 34394034
Staphylococcus aureus α-toxin induces acid sphingomyelinase release from a human endothelial cell line [ bioRxiv, 2021, 10.1101/2021.03.29.437456]	PubMed: None
Partial Reduction of Amyloid β Production by β-Secretase Inhibitors Does Not Decrease Synaptic Transmission [ Alzheimers Res Ther, 2020, 26;12(1):63]	PubMed: 32456694

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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