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

Wortmannin Chemical Structure

CAS: 19545-26-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1392.31 现货
5mg RMB 899.84 现货
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批次: 纯度: 99.97%
99.86

Wortmannin相关产品

相关信号通路图

PI3K抑制剂选择性比较

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
Mel-HO Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
A-375-TS  Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
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
BEL/FU Function Assay 1 mM 24 h decreases protein levels of the PI3K/Akt pathway 24232099
HCT 116  Function Assay 100 nM 24 h attenuates the colonies of the tumor cells with upregulation of Akt1 24297510
HepG2 Function Assay 100 nM 24 h attenuates the colonies of the tumor cells with upregulation of Akt1 24297510
SW480  Function Assay 150nM 20 h reduces cellular accumulation of β-catenin 24324366
HEK-293 Function Assay 150nM 16 h decreases CRT activity 24324366
5637 Apoptosis Assay 10 μM 40 min reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan 24333868
MG-63 Apoptosis Assay 10 µM 12 h enhances DP-induced apoptosis 24358301
H1975 Function Assay 10 μM 1 h decreases cellular phospho-AKT protein levels 24447935
H520 Function Assay 10 μM 1 h decreases cellular phospho-AKT protein levels 24447935
HepG2  Function Assay 200 nM 0.5 h attenuates FoxO phosphorylation 24535192
HL-60 Function Assay 0.1 μM 72 h blocks dasatinib-induced cell differentiation 24607273
SK-N-LO Function Assay 100 nM 0.5 h decreases the stimulant effects of morphine on Akt phosphorylation 24654606
A549  Function Assay 10 μm  16 h modulates the IAV replication and causes retention of NP in the nucleus. 24802111
A549  Growth Inhibition Assay 3 µM  2 h suppresses pemetrexed-induced Akt and GSK3β activation, S-phase arrest, cell apoptosis and caspase-3 activation 24847863
HepG2 Function Assay 100 nM 0.5 h blocks MA-induced Akt phosphorylation 24863350
MO59J Apoptosis Assay 10 μM 24 h increases the DSB level induced by etoposide or cisplatin 24953561
MO59K  Apoptosis Assay 10 μM 24 h increases the DSB level induced by etoposide or cisplatin 24953561
MO59J Cytotoxicity Assay 5 μM 7 d enhances the cytotoxicity of etoposide or cisplatin 24953561
MO59K  Cytotoxicity Assay 5 μM 7 d enhances the cytotoxicity of etoposide or cisplatin 24953561
HT-29  Growth Inhibition Assay 1.5 µM 96 h decreases cell growth which can be inhibited by KYNA 25012123
MCF7 Function Assay 100 nM 24 h eliminates E2-induced ARE-Luc activity 25172557
MDA-MB-231 Apoptosis Assay 1 μM  48 h decreases the cell survival treated with 25 μM of F1 or F2   25300932
APRE-19 Apoptosis Assay 5 μM 24 h abolishes FLZ-mediated pro-survival/anti-apoptosis activity 25329617
HUVECs Cytotoxicity Assay 100 nM 24 h attenuates the abrogative effects of calycosin on VRI-induced cytotoxicity 25450186
H1703 Growth Inhibition Assay 2.5 μM 1-4 d enhances cell growth inhibition treatment with tamoxifen 25490383
A459 Growth Inhibition Assay 2.5 μM 1-4 d enhances cell growth inhibition treatment with tamoxifen 25490383
Mel-HO-TS 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
Mel-2a Apoptosis Assay 4/8 μM 24 h enhances TRAIL-induced apoptosis  24113173
MDA-MB-231 Function Assay 0–400 nM 4 h suppresses Akt phosphorylation in a dose-dependent manner 22906259
MDA-MB-231 Function Assay 400 nM 4 h decreases MMP-9 and IL-8 protein in a dose-dependent manner 22906259
Jurkat Growth Inhibition Assay 0.25-1.25 μM 24/48 h inhibits cell proliferation 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
Jurkat Apoptosis Assay 0.25-1.25 μM 24/48 h induces cell apoptosis in both time- and dose- dependent manner 19757185
Namalwa Apoptosis Assay 0.25-1.25 μM 24/48 h induces cell apoptosis in both time- and dose- dependent manner 19757185
SW1990 Function Assay 0.01-1 μM 1 h inhibits HA-induced Akt phosphorylation 19469020
RT112  Growth Inhibition Assay 10 μM 24 h decreases the proportion of G2/M cells 18787832
MHG-U1 Growth Inhibition Assay 10 μM 24 h decreases the proportion of G2/M cells 18787832
SMMC-7721 Apoptosis Assay 200 nM 24 h increases CHX-induced apoptosis 17557191
SMMC-7721 Function Assay 200 nM 24 h up-regulates β1,4GT1 expression 17557191
HeLa Function Assay 100 nM  1 h alters the morphology of the transferrin recycling compartment 16890915
MRC5VI 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
M059J Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
HeLa Function Assay 12.5 mM 0.5 h abolishes the Ser473/Thr308 phosphorylation of AktPKB  16227394
N2a Apoptosis Assay 0.1-10 μM 2 h induces decreased cell viability in a concentration-dependent manner 15842767
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
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
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
K562 Growth Inhibition Assay 24 h IC50=25±0.14 nM 19662361
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by SRB method, IC50 = 11.4 μM. 18630894
Jurkat  Kinase Assay IC50 of 24 nM 15664519
Sf9 Function assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50 = 0.012 μM. 21121631
HeLa Function assay Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC50 = 0.049 μM. 17135248
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 Binding affinity for Phosphatidylinositol 3-kinase isolated from HeLa cells; Range is 20-120, Ki = 0.12 μM. 15658870
A549 Function assay Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot, IC50 = 0.22 μM. 17135248
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
PI3K [3]
(Cell-free assay)
DNA-PK [12]
(Cell-free assay)
ATM [12]
(Cell-free assay)
MLCK [1]
(Cell-free assay)
3 nM 16 nM 150 nM 170 nM
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]

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]

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)

体外溶解度
批次:

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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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