5.08738

Palmostatin B

InSolution, ≥95%, 50 mM in DMSO, APT1 inhibitor

• 동의어(들): InSolution APT1 Inhibitor, palmostatin B, APT1 Inhibitor
• 실험식(Hill 표기법): C₂₃H₃₆O₄
• Molecular Weight: 376.53
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: liquid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• 저장 온도: −70°C

설명

일반 설명

A cell-permeable, beta-lactone acyl protein thioesterase 1 (APT1) inhibitor (IC₅₀ = 0.67 µM, in an enzymatic assay) that is shown to specifically block Ras depalmitoylation, without affecting Ras acylation, in MDCK cells, both in vitro and in vivo. It induces a marked redistribution of NRas to endomembranes (1 µM) without notable cytotoxicity, and is shown to elicit a loss of the precise steady-state localization of palmitoylated Ras proteins in the same cell line. At 50 µM, this inhibitor displays a partial phenotypic reversion in oncogenic HRasG12V-transformed fibroblasts. Furthermore, it demonstrates selectivity for APT1 over phospholipase A1, A2, Cβ and D. It′s inhibitory effect is demonstrated to be consistent with that of APT1 downregulation by siRNA.

생화학적/생리학적 작용

Primary Target
APT1

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

물리적 형태

A 50 mM (2 mg/106.23 µL) sterile-filtered solution of APT1 Inhibitor, palmostatin B (Cat. No. 178501). in DMSO.

재구성

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -20°C.

기타 정보

Dekker, F. and Hedberg, C. 2011. Bioorg. Med. Chem. Lett.19, 1376.

Dekker, F., et al. 2010. Nat. Chem. Biol.6, 449.

법적 정보

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