(9S)-2,3,10,11,12,13-ヘキサヒドロ-3α-ヒドロキシ-10α-メトキシ-9-メチル-11α-メチルアミノ-9β,13β-エポキシ-1H,9H-ジインドロ[1,2,3-gh:3',2',1'-lm]ピロロ[3,4-j][1,7]ベンゾジアゾニン-1-オン

(9S)-2,3,10,11,12,13-ヘキサヒドロ-3α-ヒドロキシ-10α-メトキシ-9-メチル-11α-メチルアミノ-9β,13β-エポキシ-1H,9H-ジインドロ[1,2,3-gh:3',2',1'-lm]ピロロ[3,4-j][1,7]ベンゾジアゾニン-1-オン 価格

(9S)-2,3,10,11,12,13-ヘキサヒドロ-3α-ヒドロキシ-10α-メトキシ-9-メチル-11α-メチルアミノ-9β,13β-エポキシ-1H,9H-ジインドロ[1,2,3-gh:3',2',1'-lm]ピロロ[3,4-j][1,7]ベンゾジアゾニン-1-オン 化学特性,用途語,生産方法

• 説明

  UCN-01 is a synthetic derivative of staurosporine with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC₅₀ = 30 nM), PDK1 (IC₅₀ = 6 nM) and cyclin-dependent kinases (IC₅₀s = 300-600 nM for Cdk1 and Cdk2). UCN-01 arrests tumor cells in the G₁/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G₂ checkpoint kinase Chk1 (IC₅₀ = 7 nM), leading to apoptosis.

• 使用

  UCN-01 is an indolocarbazole isolated from a high staurosporine-producing Streptomyces culture. UCN-01 inhibits protein kinase C (PKC) and cyclin-dependant kinase 2 (CDK2), resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by the latter agents.

• 一般的な説明

  A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC₅₀ = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC₅₀ = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC₅₀ = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents.

(9S)-2,3,10,11,12,13-ヘキサヒドロ-3α-ヒドロキシ-10α-メトキシ-9-メチル-11α-メチルアミノ-9β,13β-エポキシ-1H,9H-ジインドロ[1,2,3-gh:3',2',1'-lm]ピロロ[3,4-j][1,7]ベンゾジアゾニン-1-オン 生産企業

Global(54)Suppliers

112953-11-4, (9S)-2,3,10,11,12,13-ヘキサヒドロ-3α-ヒドロキシ-10α-メトキシ-9-メチル-11α-メチルアミノ-9β,13β-エポキシ-1H,9H-ジインドロ[1,2,3-gh:3',2',1'-lm]ピロロ[3,4-j][1,7]ベンゾジアゾニン-1-オン キーワード