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Sotrastaurin (AEB071)

Sotrastaurin (AEB071) 是一種有效的，選擇性的泛PKC抑制劑，最有效作用于PKCθ，無細胞試驗中Ki為0.22 nM；對PKCζ沒有活性。Phase 2。

Sotrastaurin (AEB071) Chemical Structure

Sotrastaurin (AEB071) Chemical Structure

CAS: 425637-18-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1566.89 現(xiàn)貨
5mg 1414.55 現(xiàn)貨
25mg 5468.97 現(xiàn)貨
1g 32678.1 現(xiàn)貨
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細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息(PMID)
92.1 Growth Inhibition Assay 0-5 μM 72 h inhibits cell growth dose dependently 22653968
Omm1.3 Growth Inhibition Assay 0-5 μM 72 h inhibits cell growth dose dependently 22653968
Mel202 Growth Inhibition Assay 0-5 μM 72 h inhibits cell growth dose dependently 22653968
CD3+ T? Function Assay 0-500 nM 1 h inhibits NF-κB phosphorylation in a dose dependent manner 23573283
SP49 Function Assay 2.5 μM? 12 h downregulates NF-κB target genes 24362935
Rec-1 Function Assay 2.5 μM? 12 h downregulates NF-κB target genes 24362935
Mino Function Assay 2.5 μM? 12 h downregulates NF-κB target genes 24362935
Jeko-1 Function Assay 2.5 μM? 12 h downregulates NF-κB target genes 24362935
OCM3 Growth Inhibition Assay 0.5 μM 3 h increases IR-induced cell cycle arrest? 24595385
92.1 Growth Inhibition Assay 0.5 μM 3 h increases IR-induced cell cycle arrest? 24595385
Mel202 Growth Inhibition Assay 0.5 μM 3 h increases IR-induced cell cycle arrest? 24595385
OCM3 Growth Inhibition Assay 0.5 μM 3 h enhances IR-induced reduction in cell viability 24595385
92.1 Growth Inhibition Assay 0.5 μM 3 h enhances IR-induced reduction in cell viability 24595385
Mel202 Growth Inhibition Assay 0.5 μM 3 h enhances IR-induced reduction in cell viability 24595385
A549 Growth Inhibition Assay 0.1?μM 24 h enhances growth inhibition cotreated with AS-IV 25218161
A549 Function Assay 0.1?μM 24 h reduces the expression levels of MMP-2, MMP-9 and integrin β1 25218161
A549 Function Assay 0.1?μM 24 h decreases the relative PKC-α level on cell membrane cotreated AS-IV 25218161
HUVECs? Function Assay 500nM 1 h Reduces DTX-Triggered Endothelial Dysfunction 25634538
T cell Function Assay 100 nM 3 h inhibits rRNA synthesis 25691158
Mel202 Growth Inhibition Assay 5 μM 24 h induces G1 arrest? 22653968
Omm1.3 Growth Inhibition Assay 5 μM 24 h induces G1 arrest? 22653968
92.1 Growth Inhibition Assay 5 μM 24 h induces G1 arrest? 22653968
Mel202 Apoptosis Assay 5 μM 72 h induces apoptosis slightly 22653968
Omm1.3 Apoptosis Assay 5 μM 72 h induces apoptosis 22653968
92.1 Apoptosis Assay 5 μM 72 h induces apoptosis signifcantly 22653968
Mel202 Function Assay 5 μM 24 h inhibits expression and phosphorylation of PKC isoforms 22653968
Omm1.3 Function Assay 5 μM 24 h inhibits expression and phosphorylation of PKC isoforms 22653968
92.1 Function Assay 5 μM 24 h inhibits expression and phosphorylation of PKC isoforms 22653968
HBL1 Growth Inhibition Assay 0.16-20 μM 5 d IC50=0.5 μM 21324920
TMD8 Growth Inhibition Assay 0.16-20 μM 5 d IC50=0.2 μM 21324920
OCI-Ly10 Growth Inhibition Assay 0.16-20 μM 5 d IC50=1.3 μM 21324920
U2932 Growth Inhibition Assay 0.16-20 μM 5 d IC50=10 μM 21324920
OCI-Ly3 Growth Inhibition Assay 0.16-20 μM 5 d IC50＞20 μM 21324920
SuDHL2 Growth Inhibition Assay 0.16-20 μM 5 d IC50＞20 μM 21324920
SuDHL4 Growth Inhibition Assay 0.16-20 μM 5 d IC50＞20 μM 21324920
DB Growth Inhibition Assay 0.16-20 μM 5 d IC50＞20 μM 21324920
SP49 Growth Inhibition Assay 0-4 μM inhibits cell growth dose dependently 24362935
Rec-1 Growth Inhibition Assay 0-4 μM inhibits cell growth dose dependently 24362935
Mino Growth Inhibition Assay 0-4 μM inhibits cell growth dose dependently 24362935
Jeko-1 Growth Inhibition Assay 0-4 μM inhibits cell growth dose dependently 24362935
Jurkat T Function assay 5 hrs Inhibition of PKCtheta in human Jurkat T cells assessed as reduction in anti-CD3/CD28 antibody-induced T-cell activation by measuring decrease in IL-2 secretion after 5 hrs by luciferase reporter gene assay, IC50 = 0.081 μM. 28131714
bone marrow cells Antiproliferative assay 4 days Antiproliferative activity against CBA mouse bone marrow cells assessed as inhibition of [3H]thymidine incorporation after 4 days, IC50 = 3.7 μM. 19827831
Jurkat IL-2 Growth Inhibition Assay IC50=6.71 ± 3.76 μM 19940259
PBMC IL-2 Growth Inhibition Assay IC50=4.84 ± 1.70 μM 19940259
Jurkat Function assay Inhibition of TCR/CD28-mediated human T cell activation in Jurkat cells expressing human IL2 promoter by luciferase reporter gene assay, IC50 = 0.054 μM. 19827831
B-cells Function assay Inhibition of PKCbeta in mouse B cells assessed as reduction in IgM-stimulated cell proliferation, IC50 = 0.234 μM. 28131714
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生物活性

產(chǎn)品描述 Sotrastaurin (AEB071) 是一種有效的，選擇性的泛PKC抑制劑，最有效作用于PKCθ，無細胞試驗中Ki為0.22 nM；對PKCζ沒有活性。Phase 2。
特性 同以往的PKC抑制劑不同，AEB071并不會在激活誘導的細胞死亡模型中增強鼠T細胞原幼細胞的凋亡。
靶點
PKCθ
(Cell-free assay)		 PKCβ1
(Cell-free assay)		 PKCα
(Cell-free assay)		 PKCη
(Cell-free assay)		 PKCδ
(Cell-free assay)		 點擊更多
0.22 nM(Ki) 0.64 nM(Ki) 0.95 nM(Ki) 1.8 nM(Ki) 2.1 nM(Ki)
體外研究(In Vitro)
體外研究活性

在人和鼠的早期T細胞中，毫微摩爾級濃度的AEB071 (< 10μM)則能有效消除早期T細胞激活的信號如白介素-2分泌物和CD25表達。在沒發(fā)生非特異性抗增殖的效應的細胞中，AEB071 (200 nM)能抑制CD3/CD28抗體和同種抗原誘導的T瞎報增殖反應。AEB071(<3 μM)可以顯著抑制淋巴細胞功能相關抗原1介導的T細胞的粘附作用。

AEB071(< 20 μM)特異性地降低CD79突變體ABC DLBCL細胞系的增殖，隨之能減少NF-κB信號活性。3 μM 濃度的AEB071可誘導CD79突變細胞在G1阻斷和/或細胞壞死。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot p-Marcks / p-ERK / p-AKT / p-S6 / Marcks / ERK / AKT / S6

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