345885

GGTI-2147

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

• 別名: GGTI-2147, 4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
• 実験式（ヒル表記法）: C₂₈H₃₀N₄O₃
• CAS番号: 191102-87-1
• 分子量: 470.56
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• product name: GGTI-2147, A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I).
• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic)
• 色: off-white
• 溶解性: DMSO: 200 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

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).

生物化学的／生理学的作用

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)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable