P0115
PAC-1
≥98% (HPLC)
Synonym(s):
(4-Benzylpiperazino)acetic acid (3-allyl-2-hyroxybenzylidene)hydrazide, 1-Piperazineacetic acid, 2-(phenylmethyl)-,[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hyrrazide
Sign In to View Organizational & Contract Pricing.
Select a Size
Change View
About This Item
Empirical Formula (Hill Notation):
C23H28N4O2
CAS Number:
Molecular Weight:
392.49
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: ≥10 mg/mL, deionized water: ≤2 mg/mL
storage temp.
room temp
SMILES string
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+
InChI key
YQNRVGJCPCNMKT-LFVJCYFKSA-N
General description
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.
Biochem/physiol Actions
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.
Features and Benefits
This compound is featured on the Caspases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Storage Class
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Ai-Ming Zhou et al.
BMC cardiovascular disorders, 20(1), 15-15 (2020-01-15)
Platelets in patients with type 2 diabetes mellitus (DM2) are characterized by increased activation and aggregation, which tends to be associated with a high morbidity and mortality due to cardiovascular disease (CVD). Moreover, a large proportion of DM2 patients show
Procaspase-3 activation as an anti-cancer strategy: structure- activity relationship of procaspase-activating compound 1 (PAC-1) and Its cellular co-localization with caspase-3
Peterson QP et al.
Journal of Medicinal Chemistry, 52(18), 5721-5731 (2009)
Yingxue Qi et al.
Journal of hematology & oncology, 11(1), 117-117 (2018-09-19)
Platelet glycoprotein Ibα (GPIbα) extracellular domain, which is part of the receptor complex GPIb-IX-V, plays an important role in tumor metastasis. However, the mechanism through which GPIbα participates in the metastatic process remains unclear. In addition, potential bleeding complication remains