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Merck
CN
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主要文件

345885

Sigma-Aldrich

GGTI-2147

≥95% (HPLC), solid, GGTase I inhibitor, Calbiochem®

别名:

GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester

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About This Item

经验公式(希尔记法):
C28H30N4O3
分子量:
470.56
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).

质量水平

方案

≥95% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)

颜色

off-white

溶解性

DMSO: 200 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

[nH]1cnc(c1)CNc2cc(c(cc2)C(=O)N[C@@H](CC(C)C)C(=O)OC)c3c4c(ccc3)cccc4

InChI key

TUQRZGWNDBXSNP-SANMLTNESA-N

一般描述

A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I). Blocks the geranyl-geranylation of Rap1A with an IC50 value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50 >30 µM for H-Ras).
Methyl ester derivative of GGTI-2133 (Cat. No. 345884). A potent and selective non-thiol inhibitor of geranylgeranyltransferase I (GGTase I) over farnesyltransferase (FTase) in whole cells. Blocks the geranylgeranylation of Rap1A with an IC50 value greater than 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50<30 µM for H-Ras).

生化/生理作用

Cell permeable: yes
Primary Target
GGTase-I
Product does not compete with ATP.
Reversible: no
Target IC50: 500 nM in blocking the geranyl-geranylation of Rap1A

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol.41, 316.
Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 1

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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