LY294002 | SF 1101 | PI3K Inhibitor | AmBeed-信号通路专用抑制剂

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LY294002 99%+

货号：A133122 同义名： SF 1101;NSC 697286

LY294002 是一种 PI3K 抑制剂，抑制 PI3Kα, PI3Kδ 和 PI3Kβ 的 IC50 分别为 0.5, 0.57, 0.97 μM。LY294002 具有抗肿瘤作用，可用于研究 PI3K/AKT 信号通路和相关癌症治疗。

LY294002 化学结构
CAS号：154447-36-6

LY294002 3D分子结构
CAS号：154447-36-6

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LY294002 纯度/质量文件产品仅供科研

货号：A133122 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

PI3K 亚型比较
自噬亚型比较
Casein Kinase 亚型比较

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%+
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%+
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	99%+
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%+
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%+
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	99%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				99%+
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%+
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			99%+
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				99%+
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	99%+
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	99+%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%+
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	99%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	99%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					99%+
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				99%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				99%+
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				98%+
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Src,Sirtuin,PKC	97%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%+
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%+
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%+
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				99+%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%+
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%+
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		MLCK,DNA-PK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	99%+
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	98%
α-Linolenic acid						✔			97% GC
MTX-211						✔		EGFR	99%+
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		99%+
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		99%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		99%+
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	CK1 ↓ ↑	CK2 ↓ ↑	其他靶点	纯度
PF-670462 2HCl	++++ CK1ε, IC50: 90 nM CK1δ, IC50: 13 nM			99%+
D4476	++ CK1 from Schizosaccharomyces pombe, IC50: 200 nM CK1δ, IC50: 300 nM			99%+
SR-3029	+++ CK1ε, IC50: 260 nM CK1δ, IC50: 44 nM			99%+
IWP-2	+++ ^M82FCK1δ, IC50: 40 nM		Wnt	99%+
LY364947	++ CK1δ, IC50: 0.22 μM			98%
TA-01	++++ CK1ε, IC50: 6.4 nM CK1δ, IC50: 6.8 nM		p38 MAPK	99%+
IC261	+ CK1, IC50: 16 μM			99%+
PF-4800567	+++ casein kinase 1 delta, IC50: 711 nM casein kinase 1 epsilon, IC50: 32 nM			99%+
CK1-IN-1	++++ CK1ε, IC50: 16 nM CK1δ, IC50: 15 nM			99%+
Longdaysin	+ CKIα, IC50: 5.6 μM CKIδ, IC50: 8.8 μM			99%+
Silmitasertib		++++ CK2, IC50: 1 nM		99%+
Ellagic acid (hydrate)		+++ CK2, IC50: 0.04 μM	PKA	95+%
DMAT		+++ CK2, Ki: ~40 nM		99%+
Hematein		++ CK2, IC50: 0.55 μM		98+%
Silmitasertib sodium salt		++++ CK2α', IC50: 1 nM CK2α, IC50: 1 nM		99%+
LY294002		+++ CK2, IC50: 98 nM		99%+
A-3 HCl	+ CK1, Ki: 80 μM	++ CK2, Ki: 5.1 μM	PKA,MLCK,PKC	98+%
TBB	+ CK1, Ki: 47 μM	++ CK2, Ki: 0.4 μM		99%+
TTP 22		++ CK2, IC50: 100 nM		98%+
DRB		✔		99%+
BioE-1115		+ CK2α, IC50: 10 μM		99%+
(E/Z)-GO289		++++ CK2, IC50: 7 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

LY294002 生物活性

靶点	p110β p110β, IC50:0.97 μM p110α p110α, IC50:0.5 μM p110δ p110δ, IC50:0.57 μM CK2 CK2, IC50:98 nM
描述	PI3Ks (Phosphatidylinositol-4,5-bisphosphate 3-kinase) participate in a diverse array of process, including the regulation of cellular survival, differentiation and stem cell-like properties, growth, proliferation, metabolism, migration, and angiogenesis^[2]. LY294002 is the first synthetic molecule to inhibit p110α, p110β and p110δ, which is the 110 kDa catalytic subunit of class IA PI3Ks, with IC50 value of 0.5 μM, 0.57 μM, 0.97 μM (determined using the PI3K lipid kinase assays on recombinant protein), respectively^[1]. LY294002 can induce apoptosis of human nasopharyngeal carcinoma in vitro and in vivo^[3], induce a senescence-like growth arrest in human diploid fibroblasts^[4], decrease invasion and migration of human ovarian carcinoma cells^[5]. Also it can be used as an autophagy inhibitor^[6].
作用机制	LY294002 acts at the ATP-binding site of the PI3Ks enzyme.^[7]

LY294002 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay	1.5 h	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	22537153
HeLa (human carcinoma) cells.		Function assay		In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM.	15658870
HeLa cells		Function assay		Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870
HeLa cells		Function assay		Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248

LY294002 动物研究

Dose	Mice: 0 - 100 mg/kg^[1] Rats: min = 50 mg/kg^[2], max = 100 mg/kg^[3]
Administration	i.p.

LY294002 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02337309	Neuroblastoma	Phase 1	Terminated(Low patient accrual... 展开 >>) 收起 <<	-	United States, California ... 展开 >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027-0700 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94143 United States, Colorado Children Hospital of Colorado Aurora, Colorado, United States, 80045 United States, Georgia AFLAC Cancer Center and Blood Disorders Service of Children's Healthcare of Atlanta - Egleston Campus Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Comer Children's Hospital Chicago, Illinois, United States, 60637 United States, Massachusetts Childrens Hospital Boston, Dana-Farber Cancer Institute. Boston, Massachusetts, United States, 02115 United States, Michigan C.S Mott Children's Hospital Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229-3039 United States, Texas Cook Children's Healthcare System Fort Worth, Texas, United States, 76104 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 收起 <<

LY294002 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.54mL

6.51mL

3.25mL

LY294002 技术信息

CAS号	154447-36-6
分子式	C₁₉H₁₇NO₃
分子量	307.343

别名	SF 1101;NSC 697286
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(162.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(162.68 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验配方

5% DMSO+ 40%PEG 300+5% Tween 80+50%water 3 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

HEK293 cells		Function assay	1.5 h	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	22537153
HeLa (human carcinoma) cells.		Function assay		In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM.	15658870
HeLa cells		Function assay		Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870
HeLa cells		Function assay		Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248
HeLa cells		Binding affinity assay		Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM	15658870
human 184B5 cells		Cytotoxic assay		Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM.	18691894
human A2780 cells	2 μM	Apoptosis assay	12 h	Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis.	17684018
human A375 cells		Proliferation assay	46 h	Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM.	17049248
human A375 cells		Proliferation assay		Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM.	17601739
human A549 cells		Proliferation assay	72 h	Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM.	25693787
human A549 cells		Cytotoxic assay	72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	22480851
human BJ cells	25 μM	Function assay	2 h	Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy	16767085
human BJ cells	25 μM	Function assay	2 h	Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting	16767085
human BT474 cell		Proliferation assay	72 h	Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis， IC50=20.7 μM.	23410005
human H1299 cells	0.1-30 μM	Function assay	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H4 cells		Function assay	2 h	Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control	18024584
human H460 cells	30 μM	Function assay		Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM	18501601
human HCT116 cells		Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM	22212721
human HCT116 cells		Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM.	22212721
human HCT116 cells		Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM.	22212721
human HCT116 cells	10 μM	Function assay	10 min	Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	10 μM	Function assay	10 min	Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	10 μM	Function assay		Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	10 μM	Function assay		Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	10 μM	Function assay		Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis	22212721
human HCT116 cells		Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM.	25693787
human HCT116 cells		Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM.	21945250
human HL60 cells		Cytotoxic assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM.	22480851
human HL60 cells		Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM.	25693787
human HuH7 cells		Proliferation assay	72 h	Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM.	25693787
human IGROV1 cells		Function assay	24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human IGROV1 cells		Function assay	24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human IGROV1 cells		Function assay	24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry	21216151
human IGROV1 cells		Function assay	24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry	21216151
human KB cells		Cytotoxic assay	72 h	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM.	21945250
human LNCAP cells	0.1-30 μM	Function assay	30 min	Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis	22832316
human LNCAP cells	0.1-30 μM	Function assay	24 h	Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22832316
human MCF7 cells		Cytotoxic assay		Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM.	18691894
human MCF7 cells		Cytotoxic assay		Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM.	18691894
human MCF7 cells		Cytotoxic assay		Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM.	18691894
human MDA-MB-231 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM.	18691894
human MDA-MB-231 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM.	18691894
human MDA-MB-468 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay， IC50=4.76 μM.	18691894
human MDA-MB-468 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM.	18691894
human MDA-MB-468 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM.	18691894
human MGC803 cells	25 μM	Function assay	48 h	Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control	24119869
human PC3 cell		Proliferation assay	72 h	Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM.	23410005
human PC3 cells		Function assay	30 min	Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM.	23410005
human PC3 cells	50 μM	Function assay	8 h	Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control	22998472
human PC3 cells		Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM.	22480851
human PC3 cells	25 μM	Proliferation assay	120 h	Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO	16680159
human SW480 cells	20 μM	Function assay	24 h	Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis	17472962
human U251HRE cells		Function assay		Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay	18501601
human U87MG cells		Function assay		Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM.	18345609
HUVEC	10-25 μM	Function assay	16 h	Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis	22026410
HUVEC	10-25 μM	Function assay	30 min	Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay	22026410
MDA-MB-231 cells		Cell invasion assay	24 h	Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM.	22804108
MDA-MB-231 cells		Cytotoxic assay		Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM.	18691894
mouse mast cells	20 μM	Function assay		Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM	16789742
mouse Raw264 macrophage		Function assay		Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM.	16789742
mouse RAW264.7 cells	25 μM	Function assay	20 h	Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis	24299616
rat RBL2H3 cells		Function assay		Inhibition of A23187-induced degranulation in rat RBL2H3 cells	18328716
Sf21 cells		Function assay		Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50=0.5 μM	22520630
Sf21 cells		Function assay		Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM.	19748269
Sf9 cells		Fluorescent polarization assay		Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM.	21121631
Sf9 cells		Function assay		Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM.	18321716
Sf9 cells		Function assay		Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM.	10998351
Sf9 cells		fluorescent polarization assay		Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay	21121631
THP1 cells		Function assay		Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM.	16789742
THP1 cells		Function assay		Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM.	16789742
THP1 cells		Function assay		Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM.	16789742

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p110β	p110β, IC50:0.97 μM
p110α	p110α, IC50:0.5 μM
p110δ	p110δ, IC50:0.57 μM
CK2	CK2, IC50:98 nM

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