Wortmannin

别名: KY 12420, SL-2052, BRN 0067676, NSC 627609 中文名称：渥曼青霉素

目录号：S2758 Purity: 99.97%

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

规格	价格	库存
10mM (1mL in DMSO)	RMB 1392.31	现货
5mg	RMB 899.84	现货
20mg	RMB 2375.66	现货
更大包装
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客户使用Selleck的Wortmannin发表文献307篇

产品质控

批次：纯度： 99.97%

99.97

Wortmannin相关产品

相关靶点	p110α p110β p110δ p110γ C2β Vps34	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库凋亡分子化合物库细胞周期化合物库 NF-κB信号通路库	点击展开

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

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

参考文献
[1] Nakanishi S, et al. J Biol Chem, 1992, 267(4), 2157-2163. [2] Arcaro A, et al. Biochem J, 1993, 296(Pt 2), 297-301. [3] Yano H, et al. J Biol Chem, 1993, 268(34), 25846-25856. [4] Okada T, et al. J Biol Chem, 1994, 269(5), 3568-3573. [5] Zeng G, et al. J Clin Invest, 1996, 98(4), 894-898. [6] Boulton S, et al. Carcinogenesis, 1996, 17(11), 2285-2290. [7] Liu Y, et al. Chem Biol, 2005, 12(1), 99-107. [8] Hazeki K, et al. Mol Pharmacol, 2006, 69(5), 1717-1724. [9] Liu Y, et al. J Biol Chem, 2007, 282(4), 2505-2511. [10] Teranishi F, et al. Cancer Sci, 2009, 100(4), 770-777. [11] Ng SS, et al. Clin Cancer Res, 2001, 7(10), 3269-3275. [12] Sarkaria JN, et al. Cancer Res, 1998, 58(19), 4375-4382. [13] Ma S, et al. Proc Natl Acad Sci U S A. 2022 Jan 18;119(3):e2114134119. + 展开

参考文献

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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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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