P0115

PAC-1

≥98% (HPLC)

• 別名: (4-Benzylpiperazino)acetic acid (3-allyl-2-hyroxybenzylidene)hydrazide, 1-Piperazineacetic acid, 2-(phenylmethyl)-,[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hyrrazide
• 実験式（ヒル表記法）: C₂₃H₂₈N₄O₂
• CAS番号: 315183-21-2
• 分子量: 392.49
• MDL番号: MFCD03302441
• UNSPSCコード: 12352200
• PubChem Substance ID: 329820019
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• 色: white
• 溶解性: DMSO: ≥10 mg/mL; deionized water: ≤2 mg/mL
• 保管温度: room temp
• SMILES記法: 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

詳細

詳細

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.

生物化学的／生理学的作用

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.

特徴および利点

This compound is featured on the Caspases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 個人用保護具 (PPE): dust mask type N95 (US), Eyeshields, Gloves