345878

GGTI-286

A potent, cell-permeable, and selective inhibitor of GGTase I.

• 동의어(들): GGTI-286, N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
• 실험식(Hill 표기법): C₂₃H₃₁N₃O₃S
• CAS Number: 171744-11-9
• Molecular Weight: 429.58
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥90% (HPLC)
• 형태: solid (Glassy)
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze
• solubility: DMSO: 10 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

A potent, cell-permeable, and selective GGTase-I inhibitor. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is 25-fold more potent (IC₅₀ = 2 µM versus 50 µM) than FTI-277 (Cat. No. 344555) inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.

A potent, cell-permeable, and selective inhibitor of GGTase I. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is about 25-fold more potent (IC₅₀ = 2 µM vs. 50 µM) than FTI-277 (Cat. No. 344555) in inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Geranylgeranyltransferase (GGTase)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2 µM against GGTase

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

물리적 형태

Supplied as a trifluoroacetate salt.

재구성

Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.

기타 정보

Bredel, M., et al. 1998. Neurosurgery 43, 124.
Qian, Y., et al. 1998. Bioorg. Med. Chem.6, 293.
Lerner, E.C., et al. 1997. Oncogene 15, 1283.
Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.

법적 정보

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

안전성 정보

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable