- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
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(wú)細(xì)胞試驗(yàn)中Ki為0.22 nM；對(duì)PKCζ沒(méi)有活性。Phase 2。
Sotrastaurin (AEB071) Chemical Structure
CAS: 425637-18-9
產(chǎn)品質(zhì)控
批次：
純度：
99.97%
99.97
Sotrastaurin (AEB071)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ PKCι | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | Go 6983 Enzastaurin Bisindolylmaleimide I (GF109203X) PMA (Phorbol 12-myristate 13-acetate) Go6976 Bisindolylmaleimide IX (Ro 31-8220) Mesylate Ruboxistaurin (LY333531) Hydrochloride Rottlerin PKC-theta inhibitor Chelerythrine Chloride (NSC 646662) Darovasertib (LXS-196) Dequalinium Chloride Myricitrin Epsilon-V1-2 VTX-27 Chelerythrine | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) MAPK抑制劑庫(kù) 細(xì)胞周期化合物庫(kù) TGF-beta/Smad信號(hào)通路庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類(lèi)型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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(wú)細(xì)胞試驗(yàn)中Ki為0.22 nM；對(duì)PKCζ沒(méi)有活性。Phase 2。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | 同以往的PKC抑制劑不同，AEB071并不會(huì)在激活誘導(dǎo)的細(xì)胞死亡模型中增強(qiáng)鼠T細(xì)胞原幼細(xì)胞的凋亡。 | |||||||||||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||||
| 體外研究活性 | 在人和鼠的早期T細(xì)胞中，毫微摩爾級(jí)濃度的AEB071 (< 10μM)則能有效消除早期T細(xì)胞激活的信號(hào)如白介素-2分泌物和CD25表達(dá)。在沒(méi)發(fā)生非特異性抗增殖的效應(yīng)的細(xì)胞中，AEB071 (200 nM)能抑制CD3/CD28抗體和同種抗原誘導(dǎo)的T瞎報(bào)增殖反應(yīng)。AEB071(<3 μM)可以顯著抑制淋巴細(xì)胞功能相關(guān)抗原1介導(dǎo)的T細(xì)胞的粘附作用。[1] AEB071(< 20 μM)特異性地降低CD79突變體ABC DLBCL細(xì)胞系的增殖，隨之能減少NF-κB信號(hào)活性。3 μM 濃度的AEB071可誘導(dǎo)CD79突變細(xì)胞在G1阻斷和/或細(xì)胞壞死。[2] |
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| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID | ||
| Western blot |
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