추천 제품
분석
≥98% (HPLC)
형태
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. 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.
생화학적/생리학적 작용
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
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
이미 열람한 고객
Targeting of C-type lectin-like receptor 2 or P2Y12 for the prevention of platelet activation by immunotherapeutic CpG oligodeoxynucleotides: comment.
Journal of thrombosis and haemostasis : JTH, 16(1), 181-185 (2017-10-21)
Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1)
ACS Combinatorial Science, 14(1), 44-50 (2011)
Arterial thrombosis in the context of HCV-associated vascular disease can be prevented by protein C.
Cellular & molecular immunology, 14(12), 986-996 (2016-04-19)
Hepatitis C virus (HCV) infection is a major problem worldwide. HCV is not limited to liver disease but is frequently complicated by immune-mediated extrahepatic manifestations such as glomerulonephritis or vasculitis. A fatal complication of HCV-associated vascular disease is thrombosis. Polyriboinosinic:polyribocytidylic
International journal of biological macromolecules, 106, 878-884 (2017-08-27)
The primary biological function of platelets is to form hemostatic thrombi that prevent blood loss and maintain vascular integrity. These multi-responding cells are activated by different endogenous, physiological agonists due to the vast number of receptors present on the surface
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
Journal of Medicinal Chemistry, 52(18), 5721-5731 (2009)
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