P0115

PAC-1

≥98% (HPLC)

• Sinónimos: (4-Benzylpiperazino)acetic acid (3-allyl-2-hyroxybenzylidene)hydrazide, 1-Piperazineacetic acid, 2-(phenylmethyl)-,[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hyrrazide
• Fórmula empírica (notación de Hill): C₂₃H₂₈N₄O₂
• Número de CAS: 315183-21-2
• Peso molecular: 392.49
• Número MDL: MFCD03302441
• Código UNSPSC: 12352200
• ID de la sustancia en PubChem: 329820019
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: solid
• color: white
• solubilidad: DMSO: ≥10 mg/mL; deionized water: ≤2 mg/mL
• temp. de almacenamiento: room temp
• cadena SMILES: Oc1c(CC=C)cccc1\C=N\NC(=O)CN2CCN(CC2)Cc3ccccc3
• InChI: 1S/C23H28N4O2/c1-2-7-20-10-6-11-21(23(20)29)16-24-25-22(28)18-27-14-12-26(13-15-27)17-19-8-4-3-5-9-19/h2-6,8-11,16,29H,1,7,12-15,17-18H2,(H,25,28)/b24-16+
• Clave InChI: YQNRVGJCPCNMKT-LFVJCYFKSA-N

Descripción

Descripción general

Procaspase-activating compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazine compound. It is cytotoxic to a variety of cancer cells, such as lymphoma, leukaemia, breast carcinoma and glioblastoma. High doses of PAC-1 can promote neuroexcitation. It helps in the in vitro autoactivation of the proenzyme protease, which acts as a prototype for other protease activating compounds. PAC-1 dependant activation of procaspase-3 is associated with the chelation of zinc.

Acciones bioquímicas o fisiológicas

PAC-1 is a caspase 3 activator. Caspase activation is a key strategy in cancer therapy. Caspase 3 is a key executioner caspase and direct effector of apoptosis. Hallmark of many cancers is the circumvention of signal in the activation of executioner caspases and loss of apoptotic response. EC₅₀ for caspase 3 activation = 0.33 μM and caspase 7= 4.5 μM. The IC₅₀ for apoptosis induction = 0.92 μM. Elevated caspase 3 level in cancerous cell lines and tissues allows PAC-1 to selectively induce apoptosis in tissues.

Características y beneficios

This compound is featured on the Caspases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Equipo de protección personal: dust mask type N95 (US), Eyeshields, Gloves