GI254023X

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.

CAS No. 260264-93-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 38800	国内在庫あり
2mg	JPY 22000	国内在庫あり
5mg	JPY 32500	国内在庫あり
25mg	JPY 100500	国内在庫あり
100mg	JPY 253500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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製品安全説明書

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GI254023X関連製品

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Immunology & Inflammation related阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
L428	Function assay	24 hrs	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=5μM.	26871660
L540	Function assay	24 hrs	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=7μM.	26871660
KM-H2	Function assay	24 hrs	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=10μM.	26871660
KM-H2	Function assay	24 hrs	Inhibition of ADAM-17 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA, IC50=10μM.	26871660
KM-H2	Function assay	24 hrs	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=10μM.	26871660
L428	Function assay	24 hrs	Inhibition of ADAM-17 in human L428 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA, IC50=10μM.	26871660
L540	Function assay	24 hrs	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=10μM.	26871660
KM-H2	Function assay	24 hrs	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM.	26871660
L428	Function assay	24 hrs	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM.	26871660
L540	Function assay	24 hrs	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM.	26871660
L428	Function assay	24 hrs	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=15μM.	26871660
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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.

Targets

ADAM10 ^[1]
(Cell-free assay)

5.3 nM

In Vitro
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].
細胞実験	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.

In Vivo
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].
動物実験	動物モデル	BALB/c mice
	投与量	200 mg/kg
	投与経路	i.p.

参考
[1] Herzog C, et al. J Biol Chem. 2014, 289(19):13308-22. [2] Ludwig A, et al. Comb Chem High Throughput Screen. 2005, 8(2):161-71. [3] Schmidt S, et al. J Exp Med. 2018, 215(4):1205-1225. [4] Powers ME, et al. J Infect Dis. 2012, 206(3):352-6. [5] Shackleton B, et al. Fluids Barriers CNS. 2016, 13(1):14. [6] Metz VV, et al. PLoS One. 2012;7(7):e41823. + 展開

参考

+ 展開

化学情報

分子量	391.50	化学式	C₂₁H₃₃N₃O₄
CAS No.	260264-93-5	SDF	--
Smiles	CC(C(CCCC1=CC=CC=C1)C(=O)NC(C(=O)NC)C(C)(C)C)N(C=O)O
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 79 mg/mL ( (201.78 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 79 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):