537076

Proprotein Convertase Inhibitor

The Proprotein Convertase Inhibitor controls the biological activity of Proprotein Convertase. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• 동의어(들): Proprotein Convertase Inhibitor, PACE4 Inhibitor, Furin-like Proprotein Convertase Inhibitor, Furin Inhibitor III, PC1/3 Inhibitor, PC4 Inhibitor, PC5/6 Inhibitor
• 실험식(Hill 표기법): C₃₅H₅₅N₁₅O₄
• Molecular Weight: 749.91
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 효능: 16 pM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 100 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

A cell-permeable tripeptide derivative containing an Arg-X-Arg motive that acts as a highly potent and reversible furin inhibitor (K_i = 16 pM). Also shown to inhibit several other pro-protein convertases, such as PC1/3, PC4, PAEC4, PC5/6 with almost similar potency, but does not affect PC2, PC7, and trypsin-like serine proteases in any significant manner. Acts as a very weak inhibitor of plasmin (K_i = 7.3 µM). Exhibits greater stability in cells. Shown to block hemagglutinin cleavage (40% at 1 µM) and fowl plague virus (FPV) viral propagation in a dose-dependent manner. Exhibits minimal toxicity even at high concentrations (25-50 µM) and protects human epidermoid carcinoma (HEp-2) cells from toxic effects of Shiga toxin.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Furin, PAEC4, PC1/3, PC4, and PC5/6

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

물리적 형태

Supplied as a trifluoroacetate salt.

재구성

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

기타 정보

Becker, G., et al. 2012. J Biol Chem287, 21992.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable