P0115

PAC-1

≥98% (HPLC)

• Sinonimo/i: (4-Benzylpiperazino)acetic acid (3-allyl-2-hyroxybenzylidene)hydrazide, 1-Piperazineacetic acid, 2-(phenylmethyl)-,[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hyrrazide
• Formula empirica (notazione di Hill): C₂₃H₂₈N₄O₂
• Numero CAS: 315183-21-2
• Peso molecolare: 392.49
• Numero MDL: MFCD03302441
• Codice UNSPSC: 12352200
• ID PubChem: 329820019
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Stato: solid
• Colore: white
• Solubilità: DMSO: ≥10 mg/mL; deionized water: ≤2 mg/mL
• Temperatura di conservazione: room temp
• Stringa SMILE: 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+; YQNRVGJCPCNMKT-LFVJCYFKSA-N

Descrizione

Descrizione generale

Procaspase-activating compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazine compound.[1] It is cytotoxic to a variety of cancer cells, such as lymphoma, leukaemia, breast carcinoma and glioblastoma.[2] High doses of PAC-1 can promote neuroexcitation.[2] It helps in the in vitro autoactivation of the proenzyme protease, which acts as a prototype for other protease activating compounds.[3] PAC-1 dependant activation of procaspase-3 is associated with the chelation of zinc.[1]

Azioni biochim/fisiol

PAC-1 is a caspase 3 activator.

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.

Caratteristiche e vantaggi

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Dispositivi di protezione individuale: dust mask type N95 (US), Eyeshields, Gloves