- 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
- 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
Home
PI3K/Akt/mTOR
PI3K inhibitor
-
ATM/ATR inhibitor
-
Autophagy inhibitor
-
DNA-PK inhibitor
-
Autophagy inhibitor
-
PLK inhibitor
Wortmannin
僅限科研使用
Wortmannin
別名: KY 12420, SL-2052, BRN 0067676, NSC 627609 中文名稱：渥曼青霉素
Wortmannin是一種首次命名的PI3K抑制劑，在無細(xì)胞試驗(yàn)中IC50為3 nM，對(duì) PI3K 家族的選擇性較低。Wortmannin 可抑制自噬體的形成，并有效抑制DNA-PK/ATM，在無細(xì)胞試驗(yàn)中IC50為16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。
Wortmannin Chemical Structure
CAS: 19545-26-7
產(chǎn)品質(zhì)控
批次：
純度：
99.97%
99.97
Wortmannin相關(guān)產(chǎn)品
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)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| MDA-MB-231 | Function assay | 1 to 10 uM | 24 hrs | Inhibition of PI3K in human MDA-MB-231 cells assessed as inhibition of AKT phosphorylation at 1 to 10 uM after 24 hrs by Western blot analysis | 24828286 |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by SRB method, IC50 = 11.4 μM. | 18630894 | |
| A549 | Function assay | Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot, IC50 = 0.22 μM. | 17135248 | ||
| HeLa | Function assay | Binding affinity for Phosphatidylinositol 3-kinase isolated from HeLa cells; Range is 20-120, Ki = 0.12 μM. | 15658870 | ||
| HeLa | Function assay | Binding affinity for DNA dependent protein kinase isolated from HeLa cells; Range is 20-120, Ki = 0.12 μM. | 15658870 | ||
| HeLa | Function assay | Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC50 = 0.049 μM. | 17135248 | ||
| Sf9 | Function assay | Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50 = 0.012 μM. | 21121631 | ||
| M059J | Function Assay | 12.5 mM | 0.5 h | abolishes the Ser473/Thr308?phosphorylation of AktPKB? | 16227394 |
| AT5BIVA | Function Assay | 12.5 mM | 0.5 h | abolishes the Ser473/Thr308?phosphorylation of AktPKB? | 16227394 |
| MRC5VI | Function Assay | 12.5 mM | 0.5 h | abolishes the Ser473/Thr308?phosphorylation of AktPKB? | 16227394 |
| HeLa | Function Assay | 100?nM? | 1 h | alters the morphology of the transferrin recycling compartment | 16890915 |
| SMMC-7721 | Apoptosis Assay | 200?nM | 24 h | increases CHX-induced apoptosis | 17557191 |
| MHG-U1 | Growth Inhibition Assay | 10?μM | 24 h | decreases the proportion of G2/M cells | 18787832 |
| RT112? | Growth Inhibition Assay | 10?μM | 24 h | decreases the proportion of G2/M cells | 18787832 |
| SW1990 | Function Assay | 0.01-1 μM | 1 h | inhibits HA-induced Akt phosphorylation | 19469020 |
| Namalwa | Apoptosis Assay | 0.25-1.25 μM | 24/48 h | induces cell apoptosis in both time- and dose- dependent manner | 19757185 |
| Jurkat | Apoptosis Assay | 0.25-1.25 μM | 24/48 h | induces cell apoptosis in both time- and dose- dependent manner | 19757185 |
| Namalwa | Growth Inhibition Assay | 0.25-1.25 μM | 24/48 h | inhibits cell proliferation in both time- and dose- dependent manner | 19757185 |
| Mel-HO-TS | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| A459 | Growth Inhibition Assay | 2.5 μM | 1-4 d | enhances cell growth inhibition treatment with | 25490383 |
| H1703 | Growth Inhibition Assay | 2.5 μM | 1-4 d | enhances cell growth inhibition treatment with | 25490383 |
| HUVECs | Cytotoxicity Assay | 100 nM | 24 h | attenuates the abrogative effects of calycosin on VRI-induced cytotoxicity | 25450186 |
| MDA-MB-231 | Apoptosis Assay | 1?μM? | 48 h | decreases the cell survival treated with 25 μM of F1 or F2 ? | 25300932 |
| MCF7 | Function Assay | 100 nM | 24 h | eliminates E2-induced ARE-Luc activity | 25172557 |
| MO59K? | Cytotoxicity Assay | 5?μM | 7 d | enhances the cytotoxicity of or | 24953561 |
| MO59J | Cytotoxicity Assay | 5?μM | 7 d | enhances the cytotoxicity of or | 24953561 |
| MO59K? | Apoptosis Assay | 10 μM | 24 h | increases the DSB level induced by or | 24953561 |
| MO59J | Apoptosis Assay | 10 μM | 24 h | increases the DSB level induced by or | 24953561 |
| HepG2 | Function Assay | 100 nM | 0.5 h | blocks MA-induced Akt phosphorylation | 24863350 |
| A549? | Growth Inhibition Assay | 3 μM? | 2 h | suppresses Akt and GSK3β activation, S-phase arrest, cell apoptosis and caspase-3 activation | 24847863 |
| A549? | Function Assay | 10?μm? | 16 h | modulates the IAV replication and causes retention of NP in the nucleus. | 24802111 |
| H520 | Function Assay | 10?μM | 1 h | decreases cellular phospho-AKT protein levels | 24447935 |
| H1975 | Function Assay | 10?μM | 1 h | decreases cellular phospho-AKT protein levels | 24447935 |
| MG-63 | Apoptosis Assay | 10 μM | 12 h | enhances DP-induced apoptosis | 24358301 |
| 5637 | Apoptosis Assay | 10?μM | 40 min | reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan | 24333868 |
| HEK-293 | Function Assay | 150nM | 16 h | decreases CRT activity | 24324366 |
| BEL/FU | Function Assay | 1 mM | 24 h | decreases protein levels of the PI3K/Akt pathway | 24232099 |
| A-375 | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| Huh7? | Function Assay | 3?μM | 1 h | reduces the virus entry into the cells | 24184196 |
| A-375-TS? | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| GM00637 | Function assay | 1 uM | Inhibition of recombinant Plk3 expressed in human GM00637 cells at 1 uM assessed as decrease in p53 serine-20 phosphorylation | 17135248 | |
| Jurkat? | Kinase Assay | IC50 of 24 nM | 15664519 | ||
| N2a | Apoptosis Assay | 0.1-10 μM | 2 h | induces decreased cell viability in a concentration-dependent manner | 15842767 |
| HeLa | Function Assay | 12.5 mM | 0.5 h | abolishes the Ser473/Thr308?phosphorylation of AktPKB? | 16227394 |
| SMMC-7721 | Function Assay | 200?nM | 24 h | up-regulates β1,4GT1 expression | 17557191 |
| K562 | Growth Inhibition Assay | 24 h | IC50=25±0.14 nM | 19662361 | |
| Jurkat | Growth Inhibition Assay | 0.25-1.25 μM | 24/48 h | inhibits cell proliferation in both time- and dose- dependent manner | 19757185 |
| MDA-MB-231 | Function Assay | 400 nM | 4 h | decreases MMP-9 and IL-8 protein in a dose-dependent manner | 22906259 |
| MDA-MB-231 | Function Assay | 0–400 nM | 4 h | suppresses Akt phosphorylation in a dose-dependent manner | 22906259 |
| Mel-2a | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| MeWo | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| APRE-19 | Apoptosis Assay | 5 μM | 24 h | abolishes FLZ-mediated pro-survival/anti-apoptosis activity | 25329617 |
| HT-29? | Growth Inhibition Assay | 1.5?μM | 96 h | decreases cell growth which can be inhibited by KYNA | 25012123 |
| SK-N-LO | Function Assay | 100 nM | 0.5 h | decreases the stimulant effects of on Akt phosphorylation | 24654606 |
| HL-60 | Function Assay | 0.1?μM | 72 h | blocks cell differentiation | 24607273 |
| HepG2? | Function Assay | 200 nM | 0.5 h | attenuates FoxO phosphorylation | 24535192 |
| SW480? | Function Assay | 150nM | 20 h | reduces cellular accumulation of β-catenin | 24324366 |
| HepG2 | Function Assay | 100 nM | 24 h | attenuates the colonies of the tumor cells with upregulation of Akt1 | 24297510 |
| HCT 116? | Function Assay | 100 nM | 24 h | attenuates the colonies of the tumor cells with upregulation of Akt1 | 24297510 |
| Mel-HO | Apoptosis Assay | 4/8 μM | 24 h | enhances TRAIL-induced apoptosis? | 24113173 |
| HeLa | Function assay | 100 nM | 10 mins | Inhibition of PI3K in human HeLa cells assessed as reduction in EGF-stimulated AKT phosphorylation at S473 at 100 nM preincubated for 10 mins followed by EGF stimulation measured after 5 mins by Western blot analysis | 30380865 |
| HeLa | Function assay | 100 nM | 10 mins | Inhibition of PI3K in human HeLa cells assessed as reduction in EGF-stimulated AKT phosphorylation at T308 at 100 nM preincubated for 10 mins followed by EGF stimulation measured after 5 mins by Western blot analysis | 30380865 |
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Wortmannin是一種首次命名的PI3K抑制劑，在無細(xì)胞試驗(yàn)中IC50為3 nM，對(duì) PI3K 家族的選擇性較低。Wortmannin 可抑制自噬體的形成，并有效抑制DNA-PK/ATM，在無細(xì)胞試驗(yàn)中IC50為16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 鈣或肽底物不影響Wortmannin對(duì)MLCK的抑制，但高濃度的ATP會(huì)減弱此種抑制。Wortmannin直接與MLCK催化結(jié)構(gòu)域相互作用，導(dǎo)致不可逆轉(zhuǎn)的酶活性減弱。Wortmannin對(duì)cAMP依賴蛋白激酶，cGMP依賴的蛋白激酶，鈣調(diào)蛋白依賴激酶II，和蛋白激酶C均無抑制作用。[1] Wortmannin抑制由fMLP誘導(dǎo)的PtdInsP3（磷脂酰肌醇3,4,5-三磷酸化）形成，IC 50為5 nM 。在人中性粒細(xì)胞中，Wortmannin劑量為100 nM時(shí)可發(fā)揮完全抑制作用，增加PtdInsP2水平，且對(duì)PtdInsP和 PtdIns沒有影響；Wortmannin可動(dòng)態(tài)調(diào)控F-actin水平對(duì)fMLP刺激的肌動(dòng)蛋白聚合無影響。[2] 在RBL-2H3細(xì)胞中，Wortmannin通過結(jié)合110-kDa蛋白，不可逆的抑制磷酸肌醇3激酶(PI3-kinase)活性（IC 50為3 nM）對(duì)，對(duì)Pi4-kinase沒有影響。Wortmannin也抑制Fc epsilon RI介導(dǎo)的組胺分泌和白三烯釋放，對(duì)酪氨酸激酶Lyn無影響。[3] 在大鼠脂肪細(xì)胞中，劑量為0.1 μM的 Wortmannin可完全抑制胰島素誘導(dǎo)的己糖吸收，二不影響異丙腎上腺素刺激的脂肪分解活性。[4] 在人臍靜脈內(nèi)皮細(xì)胞中，在IGF-1的存在下，Wortmannin抑制胰島素誘導(dǎo)一氧化氮生產(chǎn)，IC50為500nM。[5] 在中國倉鼠卵巢細(xì)胞中， Wortmannin以50 μM劑量可抑制DNA雙鏈斷裂（DSB）修復(fù)，但對(duì)DSB水平無影響或單鏈斷裂（SSB）酶活無影響。Wortmannin可加強(qiáng)電離輻射（紅外）誘導(dǎo)的細(xì)胞毒作用，但本身無毒性。[6] Wortmannin抑制水球樣激酶（PLK 1）活性，IC 50為24nM，造成細(xì)胞G 2 / M阻滯。[7] 在人巨噬細(xì)胞中，Wortmannin增加 Toll樣受體（TLR）介導(dǎo)的白細(xì)胞介素- 6的積累，EC 50 = 50 nM。在小鼠巨噬細(xì)胞中，Wortmannin顯著增強(qiáng)TLR誘導(dǎo)一氧化氮合酶（iNOS）的表達(dá)和亞硝酸鹽積累。Wortmannin激活核因子-κB和上調(diào)細(xì)胞因子mRNA量。[8] Wortmannin也抑制水球樣激酶（PlK）1和PlK 3，在有絲分裂中發(fā)揮重要作用。Wortmannin治療可能導(dǎo)致可減少由DNA損傷誘導(dǎo)的p53絲氨酸20位磷酸化。[9] 在SW 1990細(xì)胞中，Wortmannin可抑制透明質(zhì)酸誘導(dǎo)Akt磷酸化和細(xì)胞運(yùn)動(dòng)/遷移。[10] |
|||
|---|---|---|---|---|
| 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 | p-AKT / AKT / p-GSK3β / GSK3β / Bcl-xl / Bax / Caspase-3 / Cleaved caspase-3 |
|
25344912 | |
| Immunofluorescence | DNMT1 |
|
24001151 | |
| Growth inhibition assay | Cell viability |
|
25344912 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Wortmannin劑量為1mg/kg可抑移植瘤小鼠中SW1990的腹膜轉(zhuǎn)移，無重量損失。[10] Wortmannin抑制在小鼠正常組織（肺，心臟和腦組織勻漿）及腫瘤組織中的phosphatidylinositide 3- B激酶（PKB）/磷酸化Akt，在劑量為0.7 mg/kg時(shí)無死亡或急性毒性。與gemcitabine聯(lián)合使用時(shí)，可大大增加細(xì)胞凋亡和抑制原位腫瘤生長(zhǎng)，兩種藥物單獨(dú)使用都無以上效果。[11] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 人胰腺癌細(xì)胞 PK1s.c.和原位注入SCID免疫缺陷小鼠。 |
| Dosages | 0.175, 0.35, 和0.7 mg/kg | |
| Administration | 靜脈注射 | |
|
化學(xué)信息&溶解度
| 分子量 | 428.43 | 分子式 | C23H24O8 |
| CAS號(hào) | 19545-26-7 | SDF | Download Wortmannin SDF |
| Smiles | CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 85 mg/mL ( (198.39 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運(yùn)輸、儲(chǔ)存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱[email protected]，直接聯(lián)系到我們。我們會(huì)在24小時(shí)內(nèi)盡快聯(lián)系您。
如果有其他問題，請(qǐng)給我們留言。
* 必填項(xiàng)
Copyright 2013 Selleck中國. All Rights Reserved.
滬ICP備13045345號(hào)-1滬公網(wǎng)安備 31011502012800號(hào)
