Wortmannin
别名: KY 12420, SL-2052, BRN 0067676, NSC 627609 中文名称：渥曼青霉素
Wortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。
Wortmannin Chemical Structure
CAS: 19545-26-7
产品质控
批次：
纯度：
99.97%
99.97
Wortmannin相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Wortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 钙或肽底物不影响Wortmannin对MLCK的抑制，但高浓度的ATP会减弱此种抑制。Wortmannin直接与MLCK催化结构域相互作用，导致不可逆转的酶活性减弱。Wortmannin对cAMP依赖蛋白激酶，cGMP依赖的蛋白激酶，钙调蛋白依赖激酶II，和蛋白激酶C均无抑制作用。[1] Wortmannin抑制由fMLP诱导的PtdInsP3（磷脂酰肌醇3,4,5-三磷酸化）形成，IC 50为5 nM 。在人中性粒细胞中，Wortmannin剂量为100 nM时可发挥完全抑制作用，增加PtdInsP2水平，且对PtdInsP和 PtdIns没有影响；Wortmannin可动态调控F-actin水平对fMLP刺激的肌动蛋白聚合无影响。[2] 在RBL-2H3细胞中，Wortmannin通过结合110-kDa蛋白，不可逆的抑制磷酸肌醇3激酶(PI3-kinase)活性（IC 50为3 nM）对，对Pi4-kinase没有影响。Wortmannin也抑制Fc epsilon RI介导的组胺分泌和白三烯释放，对酪氨酸激酶Lyn无影响。[3] 在大鼠脂肪细胞中，剂量为0.1 μM的 Wortmannin可完全抑制胰岛素诱导的己糖吸收，二不影响异丙肾上腺素刺激的脂肪分解活性。[4] 在人脐静脉内皮细胞中，在IGF-1的存在下，Wortmannin抑制胰岛素诱导一氧化氮生产，IC50为500nM。[5] 在中国仓鼠卵巢细胞中， Wortmannin以50 μM剂量可抑制DNA双链断裂（DSB）修复，但对DSB水平无影响或单链断裂（SSB）酶活无影响。Wortmannin可加强电离辐射（红外）诱导的细胞毒作用，但本身无毒性。[6] Wortmannin抑制水球样激酶（PLK 1）活性，IC 50为24nM，造成细胞G 2 / M阻滞。[7] 在人巨噬细胞中，Wortmannin增加 Toll样受体（TLR）介导的白细胞介素- 6的积累，EC 50 = 50 nM。在小鼠巨噬细胞中，Wortmannin显着增强TLR诱导一氧化氮合酶（iNOS）的表达和亚硝酸盐积累。Wortmannin激活核因子-κB和上调细胞因子mRNA量。[8] Wortmannin也抑制水球样激酶（PlK）1和PlK 3，在有丝分裂中发挥重要作用。Wortmannin治疗可能导致可减少由DNA损伤诱导的p53丝氨酸20位磷酸化。[9] 在SW 1990细胞中，Wortmannin可抑制透明质酸诱导Akt磷酸化和细胞运动/迁移。[10] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Wortmannin剂量为1mg/kg可抑移植瘤小鼠中SW1990的腹膜转移，无重量损失。[10] Wortmannin抑制在小鼠正常组织（肺，心脏和脑组织匀浆）及肿瘤组织中的phosphatidylinositide 3- B激酶（PKB）/磷酸化Akt，在剂量为0.7 mg/kg时无死亡或急性毒性。与gemcitabine联合使用时，可大大增加细胞凋亡和抑制原位肿瘤生长，两种药物单独使用都无以上效果。[11] |
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|---|---|---|
| 动物实验 | Animal Models | 人胰腺癌细胞 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 | 静脉注射 | |
化学信息&溶解度
| 分子量 | 428.43 | 分子式 | C23H24O8 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 85 mg/mL ( (198.39 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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