5.08738

Palmostatin B

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

• Synonim(y): Inhibitor APT1
• Wzór empiryczny (zapis Hilla): C₂₃H₃₆O₄
• Masa cząsteczkowa: 376.53
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: liquid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• temp. przechowywania: −70°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Primary Target
APT1

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Postać fizyczna

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

Rekonstytucja

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

Inne uwagi

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

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

Informacje prawne

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

Ta strona może zawierać tekst przetłumaczony maszynowo.