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PAC-1

PAC-1

Product ID P004080
Cas No. 315183-21-2
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $67.80 In stock
25 mg $180.30 In stock
100 mg $525.90 In stock
Bulk Quote

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  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
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  • Downloads
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Description

PAC-1 (Procaspase Activating Compound 1) has been identified through high-throughput screening as a compound that may enhance the enzymatic activity of procaspase-3 in vitro. Procaspase-3 may be useful as an anticancer strategy due to its low frequency of mutations in cancer and expression of its enzyme in several types of cancers. PAC-1 converts procaspase-3 to active caspase-3 in vitro by chelating zinc ions and thereby inducing cell death in the tumor cells. In multiple cancer cell lines, PAC-1 was shown to trigger endoplasmic reticulum stress signaling and induce autophagy and mitochondria-mediated apotosis.

Product Info

Cas No.

315183-21-2

Purity

≥98%

Formula

C23H28N4O2

Formula Wt.

392.50

Chemical Name

N'-[(6-oxo-5-prop-2-enyl-1-cyclohexa-2,4-dienylidene)methyl]-2-[4-(phenylmethyl)-1-piperazinyl]acetohydrazide

IUPAC Name

N'-[(Z)-(3-Allyl-2-hydroxyphenyl)methylene]-2-(4-benzyl-1-piperazinyl)acetohydrazide

Synonym

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

Solubility

100mM in DMSO

Appearance

White powder

Shipping and Storage

Store Temp

4°C

Ship Temp

Ambient

Downloads

MSDS

P004080 MSDS PDF

Info Sheet

P004080 Info Sheet PDF

References

Sarkar A, Balakrishnan K, Chen J, et al. Molecular evidence of Zn chelation of the procaspase activating compound B-PAC-1 in B cell lymphoma. Oncotarget. 2016 Jan 19;7(3):3461-3476. PMID: 26658105.

Roth HS, Hergenrother PJ. Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities. Curr Med Chem. 2016;23(3):201-241. PMID: 26630918.

Seervi M, Sobhan PK, Joseph J, et al. ERO1alpha-dependent endoplasmic reticulum-mitochondrial calcium flux contributes to ER stress and mitochondrial permeabilization by procaspase-activating compound-1 (PAC-1). Cell Death Dis. 2013 Dec 19;4:e968. PMID: 24357799.

Lucas PW, Schmit JM, Peterson QP, et al. Pharmacokinetics and derivation of an anticancer dosing regimen for PAC-1, a preferential small molecule activator of procaspase-3, in healthy dogs. Invest New Drugs. 2011 Oct;29(5):901-911. PMID: 20499133.

Peterson QP, Goode DR, West DC, et al. PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition. J Mol Biol. 2009 Apr 24;388(1):144-158. PMID: 19281821.

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