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Merck
모든 사진(1)

주요 문서

P0115

Sigma-Aldrich

PAC-1

≥98% (HPLC)

동의어(들):

(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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크기 선택

5 MG
₩193,967
25 MG
₩607,072

₩193,967


구입 가능 여부는 고객센터에 문의하십시오.

벌크 견적 요청

크기 선택

보기 변경
5 MG
₩193,967
25 MG
₩607,072

About This Item

실험식(Hill 표기법):
C23H28N4O2
CAS Number:
Molecular Weight:
392.49
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

₩193,967


구입 가능 여부는 고객센터에 문의하십시오.

벌크 견적 요청

분석

≥98% (HPLC)

양식

solid

색상

white

solubility

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

저장 온도

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

일반 설명

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]

생화학적/생리학적 작용

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.

특징 및 장점

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 Code

11 - Combustible Solids

WGK

WGK 3

개인 보호 장비

dust mask type N95 (US), Eyeshields, Gloves


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문서 라이브러리 방문

이미 열람한 고객

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)
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
Amelie Vallet-Courbin et al.
PloS one, 12(1), e0170305-e0170305 (2017-01-27)
Cells of the innate and adaptive immune system are key factors in the progression of atherosclerotic plaque, leading to plaque instability and rupture, potentially resulting in acute atherothrombotic events such as coronary artery disease, cerebrovascular disease and peripheral arterial disease.
Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities
Roth SH and Hergenrother JP
Current Medicinal Chemistry, 23(3), 201-241 (2016)
Patrice Marques et al.
Frontiers in immunology, 8, 1766-1766 (2018-01-13)
Cardiovascular disease (CVD) is a major comorbidity in chronic obstructive pulmonary disease (COPD). Although the mechanism of its development remains largely unknown, it appears to be associated with cigarette consumption and reduced lung function. Therefore, the aim of this study

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