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P0115

Sigma-Aldrich

PAC-1

≥98% (HPLC)

Synonim(y):

(4-Benzylpiperazino)acetic acid (3-allyl-2-hyroxybenzylidene)hydrazide, 1-Piperazineacetic acid, 2-(phenylmethyl)-,[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hyrrazide

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About This Item

Wzór empiryczny (zapis Hilla):
C23H28N4O2
Numer CAS:
315183-21-2
Masa cząsteczkowa:
392.49
Numer MDL:
MFCD03302441
Kod UNSPSC:
12352200
Identyfikator substancji w PubChem:
329820019
NACRES:
NA.77

Próba

≥98% (HPLC)

Postać

solid

kolor

white

rozpuszczalność

DMSO: ≥10 mg/mL
deionized water: ≤2 mg/mL

temp. przechowywania

room temp

ciąg 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+

Klucz InChI

YQNRVGJCPCNMKT-LFVJCYFKSA-N

Opis ogólny

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.

Działania biochem./fizjol.

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.

Cechy i korzyści

This compound is featured on the Caspases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This page may contain text that has been machine translated.

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Środki ochrony indywidualnej

dust mask type N95 (US), Eyeshields, Gloves

Certyfikaty analizy (CoA)

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