|(1S,6bR,9aS,11R,11bR)-1-(甲氧基甲基)-9a,11b-二甲基-3,6,9-三氧基-1,6,6b,7,8,9,9a,10,11,11b-十氢-3H-呋喃[4,3,2-de]茚并[4,5-h]异色烯-11-基乙酸酯|CsnPharm

CAS No.: 19545-26-7

Wortmannin/渥曼青霉素 Catalog No. CSN12216

Synonyms: SL-2052;KY-12420;渥曼青霉素

Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. It also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Phosphoinositide-3-kinase family (PI3Ks) phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role in recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. KY-12420, also termed wortmannin, is a PI3K inhibitor. The IC50 value of KY-12420 against PI3K was 3 nM according to purified calf PI3K assay or cell based immunoprecipitate assay. In intact cells, KY-12420 inhibited PI3K activity with an IC50 of 2 nM^[3]. Post 24 h incubation, KY-12420 could sensitize melanoma cell lines A375, Mel-HO, as well as respective TRAIL resistant cell lines, for TRAIL-induced apoptosis at the concentrations of 4 μM or 8 μM, as revealed by a sub-G1 cell analysis, while KY-12420 alone was not effective^[4]. In lung cancer cell lines A549 and H1703, KY-12420 at the concentration of 2.5 μM also enhanced cytotoxicity induced by tamoxifen^[5]. In an orthotopic pancreatic tumor model established by injection of PK1 cells into the pancreas of SCID mice, KY-12420 plus gemcitabine was administrated via i.p. injection. The dose of KY-12420 was 0.35 mg/kg and the dose of gemcitabine was 80 mg/kg. Both of the agents were injected biweekly for a total treatment period of 5 weeks. The result turned out that KY-12420 plus gemcitabine reduced tumor weights by 5-fold relative to the vehicle control. For comparison, the group of gemcitabine alone at the same dose and schedule reduced tumor weights by 1.4-fold, and the group of KY-12420 alone failed to inhibit tumor growth^[6].
作用机制Based on the X-ray crystallographic structure of KY-12420 bound to PI3Kγ in the kinase’s ATP binding pocket, KY-12420 most closely fits and fills the active site and induces a conformational change in the catalytic domain of the kinase^[7].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
5637	10 μM	Apoptosis Assay	40 min	reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan	24333868
A-375	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
A-375-TS	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173

更多
动物研究
剂量
Rat: 1 mg/kg^[3] (i.p.) Mice: 0.2 mg/kg - 4 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 1 mg/kg^[3] (i.p.) Mice: 0.2 mg/kg - 4 mg/kg^[4] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3341 mL
- 11.6705 mL
- 23.3409 mL
- 5 mM
- 0.4668 mL
- 2.3341 mL
- 4.6682 mL
- 10 mM
- 0.2334 mL
- 1.1670 mL
- 2.3341 mL

技术信息

CAS号

19545-26-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H24O8

运输

蓝冰

分子量

428.43

别名

SL-2052;KY-12420;渥曼青霉素

溶解度

DMSO	50.0 mg/mL (116.7 mM)
Water	insoluble

动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+water

5 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

5637	10 μM	Apoptosis Assay	40 min	reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan	24333868
A-375	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
A-375-TS	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
A459	2.5 μM	Growth Inhibition Assay	1-4 d	enhances cell growth inhibition treatment with tamoxifen	25490383
A549	3 µM	Growth Inhibition Assay	2 h	suppresses pemetrexed-induced Akt and GSK3β activation, S-phase arrest, cell apoptosis and caspase-3 activation	24847863
A549	10 μm	Function Assay	16 h	modulates the IAV replication and causes retention of NP in the nucleus.	24802111
APRE-19	5 μM	Apoptosis Assay	24 h	abolishes FLZ-mediated pro-survival/anti-apoptosis activity	25329617
AT5BIVA	12.5 mM	Function Assay	0.5 h	abolishes the Ser473/Thr308 phosphorylation of AktPKB	16227394
BEL/FU	1 mM	Function Assay	24 h	decreases protein levels of the PI3K/Akt pathway	24232099
H1703	2.5 μM	Growth Inhibition Assay	1-4 d	enhances cell growth inhibition treatment with tamoxifen	25490383
H1975	10 μM	Function Assay	1 h	decreases cellular phospho-AKT protein levels	24447935
H520	10 μM	Function Assay	1 h	decreases cellular phospho-AKT protein levels	24447935
HCT 116	100 nM	Function Assay	24 h	attenuates the colonies of the tumor cells with upregulation of Akt1	24297510
HEK-293	150nM	Function Assay	16 h	decreases CRT activity	24324366
HeLa	100 nM	Function Assay	1 h	alters the morphology of the transferrin recycling compartment	16890915
HeLa	12.5 mM	Function Assay	0.5 h	abolishes the Ser473/Thr308 phosphorylation of AktPKB	16227394
HepG2	100 nM	Function Assay	0.5 h	blocks MA-induced Akt phosphorylation	24863350
HepG2	200 nM	Function Assay	0.5 h	attenuates FoxO phosphorylation	24535192
HepG2	100 nM	Function Assay	24 h	attenuates the colonies of the tumor cells with upregulation of Akt1	24297510
HL-60	0.1 μM	Function Assay	72 h	blocks dasatinib-induced cell differentiation	24607273
HT-29	1.5 µM	Growth Inhibition Assay	96 h	decreases cell growth which can be inhibited by KYNA	25012123
Huh7	3 μM	Function Assay	1 h	reduces the virus entry into the cells	24184196
HUVECs	100 nM	Cytotoxicity Assay	24 h	attenuates the abrogative effects of calycosin on VRI-induced cytotoxicity	25450186
Jurkat	0.25-1.25 μM	Growth Inhibition Assay	24/48 h	inhibits cell proliferation in both time- and dose- dependent manner	19757185
Jurkat	0.25-1.25 μM	Apoptosis Assay	24/48 h	induces cell apoptosis in both time- and dose- dependent manner	19757185
Jurkat	-	Kinase Assay	-	IC50 of 24 nM	15664519
K562	-	Growth Inhibition Assay	24 h	IC50=25±0.14 nM	19662361
M059J	12.5 mM	Function Assay	0.5 h	abolishes the Ser473/Thr308 phosphorylation of AktPKB	16227394
MCF7	100 nM	Function Assay	24 h	eliminates E2-induced ARE-Luc activity	25172557
MDA-MB-231	1 μM	Apoptosis Assay	48 h	decreases the cell survival treated with 25 μM of F1 or F2	25300932
MDA-MB-231	0–400 nM	Function Assay	4 h	suppresses Akt phosphorylation in a dose-dependent manner	22906259
MDA-MB-231	400 nM	Function Assay	4 h	decreases MMP-9 and IL-8 protein in a dose-dependent manner	22906259
Mel-2a	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
Mel-HO	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
Mel-HO-TS	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
MeWo	4/8 μM	Apoptosis Assay	24 h	enhances TRAIL-induced apoptosis	24113173
MG-63	10 µM	Apoptosis Assay	12 h	enhances DP-induced apoptosis	24358301
MHG-U1	10 μM	Growth Inhibition Assay	24 h	decreases the proportion of G2/M cells	18787832
MO59J	5 μM	Cytotoxicity Assay	7 d	enhances the cytotoxicity of etoposide or cisplatin	24953561
MO59J	10 μM	Apoptosis Assay	24 h	increases the DSB level induced by etoposide or cisplatin	24953561
MO59K	5 μM	Cytotoxicity Assay	7 d	enhances the cytotoxicity of etoposide or cisplatin	24953561
MO59K	10 μM	Apoptosis Assay	24 h	increases the DSB level induced by etoposide or cisplatin	24953561
MRC5VI	12.5 mM	Function Assay	0.5 h	abolishes the Ser473/Thr308 phosphorylation of AktPKB	16227394
N2a	0.1-10 μM	Apoptosis Assay	2 h	induces decreased cell viability in a concentration-dependent manner	15842767
Namalwa	0.25-1.25 μM	Growth Inhibition Assay	24/48 h	inhibits cell proliferation in both time- and dose- dependent manner	19757185
Namalwa	0.25-1.25 μM	Apoptosis Assay	24/48 h	induces cell apoptosis in both time- and dose- dependent manner	19757185
RT112	10 μM	Growth Inhibition Assay	24 h	decreases the proportion of G2/M cells	18787832
SK-N-LO	100 nM	Function Assay	0.5 h	decreases the stimulant effects of morphine on Akt phosphorylation	24654606
SMMC-7721	200 nM	Apoptosis Assay	24 h	increases CHX-induced apoptosis	17557191
SMMC-7721	200 nM	Function Assay	24 h	up-regulates β1,4GT1 expression	17557191
SW1990	0.01-1 μM	Function Assay	1 h	inhibits HA-induced Akt phosphorylation	19469020
SW480	150nM	Function Assay	20 h	reduces cellular accumulation of β-catenin	24324366

Wortmannin/渥曼青霉素 Catalog No. CSN12216

靶点选择性

请登录您的专属账户

确认信息