Wortmannin | SL-2052 | PI3K Inhibitor | AmBeed-信号通路专用抑制剂

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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	98%
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	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
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			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
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	98+%
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	98%
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	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
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				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
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				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Src,PKC,Sirtuin	95%
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					✔				98%
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	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		Akt,CDK,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
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		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
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	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		95%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 HCl	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 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	ATM ↓ ↑	ATR ↓ ↑	其他靶点	纯度
Wortmannin	++ ATM, IC50: 150 nM		MLCK,DNA-PK,PI3K	99%+
CP-466722	+ ATM, IC50: 410 nM			99%+
Torin 2	++ ATM, EC50: 28 nM	++ ATR, EC50: 35 nM	DNA-PK,mTOR	99%+
KU-55933	+++ ATM, IC50: 12.9 nM			96%
ETP-46464	+ ATM, IC50: 545 nM	+++ ATR, IC50: 14 nM	DNA-PK,mTOR	98%
CGK733	++ ATM, IC50: 200 nM	++ ATR, IC50: 200 nM		99%+
AZD0156	✔			99%+
Dactolisib		+++ ATR, IC50: 21 nM		98+%
Ceralasertib		++++ ATR, IC50: 1 nM		99%+
Berzosertib		+++ ATR, IC50: 19 nM		99%+
VE-821		+++ ATR, Ki: 13 nM		99%+
AZ20		++++ ATR, IC50: 5 nM	mTOR	99%+
Schizandrin B		+ ATR, IC50: 7.25 μM	P-gp	98%
m-PEG25-NHS ester		++++ ATR, IC50: 7 nM		95%
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	DNA-PK ↓ ↑	其他靶点	纯度
PI-103	++ DNA-PK, IC50: 23 nM		99%+
CC-115	+++ DNA-PK, IC50: 0.013 μM	mTOR	98+%
Samotolisib	✔		99%+
NU 7026	+ DNA-PK, IC50: 0.23 μM	PI3K	98+%
PIK-75 HCl	++++ DNA-PK, IC50: 2 nM		99%+
PP121	+ DNA-PK, IC50: 60 nM	VEGFR,PDGFR	99%+
KU-0060648	++++ DNA-PK, IC50: 5 nM		98%
KU-57788	+++ DNA-PK, IC50: 14 nM		99%+
LTURM34	++ DNA-PK, IC50: 0.034 μM		98%+
SF2523	+++ DNA-PK, IC50: 9 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。

靶点	PI3K PI3K, IC50:3 nM ATM ATM, IC50:150 nM
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].

Cell Line rat vascular smooth muscle cells (VSMCs) rat vascular smooth muscle cells (VSMCs) NPCs HepG2 cells MDA-MB-231 cells THP-1 cells HepG2 cells	Concentration	Treated Time	Description	References
rat vascular smooth muscle cells (VSMCs)	20 µM	24 h	Inhibit PI3-kinase and block PDGF-induced downregulation of miR-145	J Am Heart Assoc. 2013 Oct 28;2(6):e000407.
rat vascular smooth muscle cells (VSMCs)	20 µM	24 h	To investigate the effect of PI3-kinase inhibitor LY294002 on PDGF-induced downregulation of miR-145 expression. Results showed that LY294002 inhibited PDGF-induced downregulation of miR-145 expression.	J Am Heart Assoc. 2013 Oct 28;2(6):e000407.
NPCs	1μM	1 hour	To simulate the phosphorylation profile of CFC NPCs and test whether these pathways are associated with accelerated cell cycle exit. Wortmannin treatment decreased phosphorylation of AKT and ERK1/2, mimicking the phenotype of CFC NPCs.	Mol Psychiatry. 2018 Aug;23(8):1687-1698.
HepG2 cells	1 µM	30 min	Wortmannin was used to inhibit PI3K activity to study its effect on LLO-induced bead internalization. The results showed that wortmannin significantly inhibited LLO-induced bead internalization.	monocytogenes into human hepatocytes. PLoS Pathog.
MDA-MB-231 cells	0.3 µM	6 h	To evaluate the effect of Wortmannin on the internalization of MDA-MB-231 cells, results showed that Wortmannin significantly decreased cellular uptake, indicating that the internalization process is PI3K-dependent.	Int J Mol Sci. 2023 Feb 10;24(4):3600.
THP-1 cells	10 μM	60 min	Wortmannin, as a PI3K inhibitor, was used to study the EMR2 activation-induced IL-8 and MMP-9 production. The results showed that Wortmannin significantly inhibited the production of IL-8 and MMP-9.	Front Immunol. 2017 Apr 3;8:373.
HepG2 cells	100 nM	30 min	Inhibition of PI 3-kinase, blocking insulin-induced upregulation of Snail1	Nat Commun. 2018 Jul 16;9(1):2751.

Species Rat Rats and mice Mice Mice	Animal Model Rat carotid artery balloon injury model Rat carotid artery balloon injury model and mouse atherosclerosis model Cav-3 overexpressing mice Ovariectomized mice	Administration	Dosage	Frequency	Description	References
Rat	Rat carotid artery balloon injury model	Intraperitoneal injection	30 µg/kg	Once daily for 3 days	Inhibit PI3-kinase and block balloon injury-induced downregulation of miR-145	J Am Heart Assoc. 2013 Oct 28;2(6):e000407.
Rats and mice	Rat carotid artery balloon injury model and mouse atherosclerosis model	Intraperitoneal injection	30 µg/kg	Once daily for 3 days	To investigate the effect of PI3-kinase inhibitor Wortmannin on balloon injury-induced downregulation of miR-145 expression. Results showed that Wortmannin significantly blocked balloon injury-induced downregulation of miR-145.	J Am Heart Assoc. 2013 Oct 28;2(6):e000407.
Mice	Cav-3 overexpressing mice	Intravenous injection	15 μg/kg	Single dose, lasting 15 minutes	Wortmannin treatment attenuated the endogenous cardiac protection observed in Cav-3 OE mice, reduced phosphorylation of Akt and GSK3β, and increased infarct size and cardiac troponin-I levels	Circulation. 2008 Nov 4;118(19):1979-88
Mice	Ovariectomized mice	Subcutaneous injection	14 µg/mouse	Single injection	Inhibit E2-induced AKT phosphorylation, thereby interfering with the induction of EGR1 and ADAMTS-1	Cell Biosci. 2021 Aug 4;11(1):155

Dose	Rat: 1 mg/kg^[3] (i.p.) Mice: 0.2 mg/kg - 4 mg/kg^[4] (i.p.)
Administration	i.p.

CAS号	19545-26-7
分子式	C₂₃H₂₄O₈
分子量	428.43
SMILES Code	CC(O[C@@H](C1=C2C(C3=C4C(C(O[C@H](COC)[C@]14C)=O)=CO3)=O)C[C@]5(C)C(CC[C@]52[H])=O)=O
MDL No.	MFCD00133927

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别名	SL-2052; KY 12420; NSC 627609; BRN 0067676; KY-12420
运输	蓝冰
InChI Key	QDLHCMPXEPAAMD-QAIWCSMKSA-N
Pubchem ID	312145

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

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