Ilomastat (GM6001)

製品コードS7157 バッチS715701

化学情報

	Synonyms	Galardin	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₈N₄O₄
	分子量	388.46	CAS No.	142880-36-2
Solubility (25°C)*	体外	DMSO	78 mg/mL (200.79 mM)
		Ethanol	8 mg/mL warmed with 50ºC water bath (20.59 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	Ilomastat (GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with K_i of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.
in vitro	GM6001 inhibits human skin fibroblast collagenase with K_i of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. ^[1] GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. ^[2]
in vivo	Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. ^[3] In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. ^[4]

製品説明

Ilomastat (GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with K_i of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.

in vitro

GM6001 inhibits human skin fibroblast collagenase with K_i of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. ^[1]

GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. ^[2]

in vivo

Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. ^[3]

In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. ^[4]

プロトコル(参考用のみ)

キナーゼアッセイ	Collagenase assay
キナーゼアッセイ	Collagenase assay uses the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. K_m is found to vary between 1.5 and 4 mM.
細胞アッセイ	細胞株	MLL cells
	濃度	20 µM
	反応時間	72 h
	実験の流れ	Cell viability was measured after 72-h exposure to triapine with co-treatment of 20 µM ilomastat
動物実験	動物モデル	Rabbit
	投薬量	100 mg/kg/day
	投与方法	subcutaneous

参考

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カスタマーフィードバック

: , , Mol Cancer, 2015, 14(1):83.

: Data from [Data independently produced by , , J Biol Chem, 2016, 291(44):22977-22987]

: Data from [Data independently produced by , , Sci Rep, 2015, 5:16951]

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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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