GM 6001

Modify Date: 2024-01-01 20:47:06

GM 6001 structure	Common Name	GM 6001
	CAS Number	142880-36-2	Molecular Weight	388.461
	Density	1.228±0.06 g/cm3	Boiling Point	N/A
	Molecular Formula	C₂₀H₂₈N₄O₄	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A

Use of GM 6001

Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.

Name	(R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide
Synonym	More Synonyms

Description	Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> MMP Research Areas >> Cancer
Target	Ki: 0.4 nM (MMP-1), 0.5 nM (MMP-2), 27 nM (MMP-3), 3.7 nM (MMP-7), 0.1 nM (MMP-8), 0.2 nM (MMP-9), 3.6 nM (MMP-12), 13.4 nM (MMP-14), 0.36 nM (MMP-26)
In Vitro	Ilomastat (GM6001) inhibits human skin fibroblast collagenase with Ki 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]. Ilomastat (0.1 nM-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, and thus inhibits T-cell homing[4].
In Vivo	Ilomastat (GM6001) (400 μg/mL) prevents corneal ulceration after severe alkali injury[2]. Ilomastat (GM6001) significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates in rabbit model after stenting[3].
Animal Admin	To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or Ilomastat (GM6001) (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. Ilomastat (GM6001) is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals are euthanized at either 1 week or 10 weeks after the second injury. For biochemical studies, iliac artery tissue is removed under general anesthetic, followed by a fatal intracardiac injection of thiopentol. For histomorphometric studies, iliac arteries are perfusion-fixed in 10% buffered formalin for 20 min at a perfusion pressure of 80 mm Hg.
References	[1]. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug 11;31(31):7152-4. [2]. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31. [3]. Li C, et al. Arterial repair after stenting and the effects of GM6001, a matrix metalloproteinase inhibitor. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8. [4]. Leppert D, et al. T cell gelatinases mediate basement membrane transmigration in vitro. J Immunol. 1995 May 1;154(9):4379-89.

Density	1.228±0.06 g/cm3
Molecular Formula	C₂₀H₂₈N₄O₄
Molecular Weight	388.461
Exact Mass	388.211060
PSA	123.32000
LogP	0.83
Appearance of Characters	Off-white solid
Index of Refraction	1.590
Storage condition	2-8°C
Water Solubility	Practically insoluble (0.062 g/L) (25 ºC)

GM 6001 MSDS(Chinese)

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases	22-24/25
RIDADR	NONH for all modes of transport
WGK Germany	3
HS Code	29339900

Precursor 8
CAS#:171347-80-1 (R)-N1-((S)-3-(... CAS#:53708-63-7 (S)-2-amino-3-(... CAS#:18908-20-8 2,5-Furandione,... CAS#:142880-34-0 methyl (R)-3-((...
CAS#:122900-21-4 boc-trp-nhme CAS#:13139-14-5 N-[(tert-Butoxy... CAS#:14035-83-7 dihydro-3-(RS)-... CAS#:162678-79-7 (2R)-2-(2-metho...
DownStream 0

Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids.

Biochemistry 31 , 7152, (1992)

The hydroxamic acid HONHCOCH2CH(i-Bu)CO-L-Trp-NHMe, isomer 6A (GM 6001), inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)...

Ilomastat

(2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide

(S-(R*,S*))-N4-Hydroxy-N{1}-(1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl)-2-(2-methylpropyl)butanediamide

GM6001

(2R)-N4-(hydroxy)-N1-((1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl)-2-(2-methylpropyl)butanediamide

Butanediamide, N-hydroxy-N-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)-, (2R)-

(2R)-N-Hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-isobutylsuccinamide

(2R)-N-Hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxo-2-propanyl]-2-isobutylsuccinamide

Galardin

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: GM 6001
Price: Click To Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: GM 6001
Price: ￥876.0/5mg ￥1466.0/10mg ￥4386.0/50mg ￥2436.0/25mg
Purity: 98.0%
Delivery: 2 Day
Contact: Liu jia
Email: 2130147988@qq.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: GM6001 (galardin, ilomastat)
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: GM6001 (galardin, ilomastat)
Price: $600.0/100mg $1100.0/250mg $2300.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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