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Merck
CN

364205

GM 6001

≥95% (HPLC), solid, Matrix metalloproteinase inhibitor, Calbiochem

别名:

GM 6001, Galardin, N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide

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关于此项目

经验公式(希尔记法):
C20H28N4O4
化学文摘社编号:
分子量:
388.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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产品名称

GM 6001, GM 6001, CAS 142880-36-2, is a potent, cell-permeable, broad-spectrum inhibitor of matrix metalloproteinases.

SMILES string

[nH]1c2c(c(c1)C[C@H](NC(=O)[C@H](CC(C)C)CC(=O)NO)C(=O)NC)cccc2

InChI

1S/C20H28N4O4/c1-12(2)8-13(10-18(25)24-28)19(26)23-17(20(27)21-3)9-14-11-22-16-7-5-4-6-15(14)16/h4-7,11-13,17,22,28H,8-10H2,1-3H3,(H,21,27)(H,23,26)(H,24,25)/t13-,17+/m1/s1

InChI key

NITYDPDXAAFEIT-DYVFJYSZSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

off-white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
MMP-1
Product does not compete with ATP.
Reversible: no
Target Ki: 400 pM for MMP-1; 500 pM for MMP-2; 27 nM for MMP-3; 100 pM for MMP-8; 200 pM for MMP-9

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, potent broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs). [Ki = 0.4 nM for skin fibroblast collagenase (MMP-1); Ki = 0.5 nM for gelatinase A (MMP-2); Ki = 27 nM for stromelysin (MMP-3); Ki = 0.1 nM for neutrophil collagenase (MMP-8); and Ki = 0.2 nM for gelatinase B (MMP-9)]. Also prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice.
A potent, cell-permeable, broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs); (Ki = 400 pM for MMP-1; Ki = 500 pM for MMP-2; Ki = 27 nM for MMP-3; Ki = 100 pM for MMP-8; and Ki = 200 pM for MMP-9). Prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice. A 10 mM (1 mg/257 µl) solution of GM6001 (Cat. No. 364206) in DMSO is also available.

Other Notes

Solorzano, C.C., et al. 1997. Shock7, 427.
Galardy, R.E., et al. 1994. Ann. NY Acad. Sci.732, 315.
Galardy, R.E., et al. 1994. Cancer Res.54, 4715.
Galardy, R.E. 1993. Drugs Future18, 1109.
Grobelny, D., et al. 1992. Biochemistry31, 7152.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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