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

规格	价格	会员价	库存	数量
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产品名称	CK1 ↓ ↑	CK2 ↓ ↑	其他靶点	纯度
PF-670462 2HCl	++++ CK1δ, IC50: 13 nM CK1ε, IC50: 90 nM			99%+
D4476	++ CK1 from Schizosaccharomyces pombe, IC50: 200 nM CK1δ, IC50: 300 nM			99%
SR-3029	+++ CK1δ, IC50: 44 nM CK1ε, IC50: 260 nM			99%+
IWP-2	+++ ^M82FCK1δ, IC50: 40 nM		Wnt	99%
LY364947	++ CK1δ, IC50: 0.22 μM			98%
TA-01	++++ CK1δ, IC50: 6.8 nM CK1ε, IC50: 6.4 nM		p38 MAPK	99%+
IC261	+ CK1, IC50: 16 μM			98%
PF-4800567	+++ casein kinase 1 epsilon, IC50: 32 nM casein kinase 1 delta, IC50: 711 nM			99%+
CK1-IN-1	++++ CK1δ, IC50: 15 nM CK1ε, IC50: 16 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		40%
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		98%
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。

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	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				mTOR,DNA-PK	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			mTOR,DNA-PK	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			mTOR,DNA-PK	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			mTOR,DNA-PK	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,Sirtuin,PKC	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						✔		PTEN,Akt	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		ATM/ATR,CDK,Akt	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		mTOR,DNA-PK	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。

Cell Line BMSCs Astrocytes TNBC cell lines HWJ-MSCs SKMEL28 melanoma cells U-251 and Ca9-22 cells ADSCs MLE-12 cells RAW 264.7 HESCs Primary chondrocytes NHA/HRasV12/TRIM24 cells Chondrocytes H9C2 cells HAEC and HSMEC Vascular Smooth Muscle Cells (VSMC) Human fetal RPE cells CTLL-2 cells RF24 cells HUVECs Human embryonic stem cells Astrocytes RAW264.7 cells BMDMs neonatal rat cardiomyocytes (NRCMs) human dental pulp stem cells PC-9R cells BMDMs A549 cells Huh7-SR cells HepG2-SR cells Mouse primary hepatocytes	Concentration	Treated Time	Description	References
BMSCs	20 µM	0, 15, 30, 60, 120 min	LY294002 significantly inhibited the higher expression of osteogenic genes induced by Ginsenoside Rb1.	Int J Oral Sci. 2022 Feb 14;14(1):10.
Astrocytes	10 µM	1 hour	AMPK inhibition reduces collective cell migration and invasion efficiency.	Nat Commun. 2022 Aug 11;13(1):4528.
TNBC cell lines	2 µM	10 days	To investigate the effect of MAPK4 knockdown on cell growth and sensitivity to PI3K inhibitors	Nat Commun. 2022 Jan 11;13(1):245.
HWJ-MSCs	40 µM	2 hours	Estimate the effects of the AKT inhibitor on the proliferation of FP2-cultured hWJ-MSCs.	J Adv Res. 2024 Aug;62:119-141.
SKMEL28 melanoma cells	20 µM	2 hours	The study involved the inhibition of AKT signaling to determine the effects on oxidative DNA damage repair; results showed reduced expression of OGG.	Redox Biol. 2024 Jun;72:103135.
U-251 and Ca9-22 cells	20 µM	2 hours	To assess the impact of PI-3 kinase inhibition on cell behavior.	Adv Sci (Weinh). 2023 Mar;10(7):e2207368.
ADSCs	50 µM	24 hours	To investigate the role of PI3K signaling on rGO/PCL induced neurotrophic phenotype changes and myelin protein secretion.	Bioact Mater. 2022 Jun 13;20:319-338.
MLE-12 cells	50 μg/mL	24 hours	LY294002 was used as a positive control to inhibit up-regulated expression of fibrosis-related genes.	J Nanobiotechnology. 2024 Oct 26;22(1):662.
RAW 264.7	10 µM	24 hours	To evaluate the effect of LY294002 on macrophage polarization.	J Nanobiotechnology. 2024 Jun 8;22(1):322.
HESCs	10 µM	24 hours	To investigate the role of LY294002 in influencing differentiation to endoderm.	Nat Commun. 2023 Jan 25;14(1):405.
Primary chondrocytes	10 µM	24 hours	LY294002 administration significantly reduced SNP-induced apoptosis activities and alleviated aberrant force-induced chondrocyte degeneration.	Int J Oral Sci. 2022 Jul 14;14(1):34.
NHA/HRasV12/TRIM24 cells	0.01 to 100 µM	24, 48, and 72 hours	Cell proliferation was evaluated and the half-maximal inhibitory concentration (IC50) values were determined from fitted concentration-response curves.	Adv Sci (Weinh). 2024 Aug;11(29):e2400023.
Chondrocytes	20 µM	3 days	The study aims to investigate the effects of blood on chondrocyte viability and apoptosis.	Signal Transduct Target Ther. 2024 May 8;9(1):109.
H9C2 cells	25 µM	30 min	To explore the mechanisms of NGR1's protective effect on H9C2 cells.	Redox Biol. 2022 Aug;54:102384.
HAEC and HSMEC	50 nM	30 min	To evaluate the effect of LY294002 on insulin uptake.	Nat Commun. 2023 Aug 17;14(1):4989.
Vascular Smooth Muscle Cells (VSMC)	50 µM	30 min	To inhibit the activation of Akt and study the effects on related signaling pathways.	Redox Biol. 2022 Jun;52:102296.
Human fetal RPE cells	2 µM	4 days	To investigate the effect of glucose concentration on inflammatory responses, where inflammatory markers were evaluated.	Nat Commun. 2022 Oct 13;13(1):6045.
CTLL-2 cells	50 µM	48 hours	The purpose was to analyze the effect of LY294002 on the CTLL-2 cells in the presence of IL-7.	Bioact Mater. 2023 Sep 26;32:12-27.
RF24 cells	50 µM	6 hours	The treatment resulted in reduced angiogenesis as inferred from subsequent experiments.	Nat Commun. 2023 Apr 26;14(1):2407.
HUVECs	5 μg/mL	6, 24, 48, and 72 hours	To observe the effects of the PI3K inhibitor as a negative control	Biomaterials. 2022 Sep;288:121729.
Human embryonic stem cells	5 µM	8 days	Induction of neuroectoderm differentiation.	Nucleic Acids Res. 2024 May 22;52(9):4935-4949.
Astrocytes	40 µM		To inhibit PI3K signaling pathway and evaluate its effects on glycophagy.	Redox Biol. 2024 Aug;74:103234.
RAW264.7 cells	25 µM	1 h	Inhibit PI3K signaling pathway and reduce M1 macrophage polarization	J Transl Med. 2024 Aug 2;22(1):717.
BMDMs	25 µM	1 h	Inhibit PI3K signaling pathway and reduce M1 macrophage polarization	J Transl Med. 2024 Aug 2;22(1):717.
neonatal rat cardiomyocytes (NRCMs)	10 μM	2 h	Inhibited PI3K α/AKT signaling, reversed FGF7-mediated promotion of Nrf2 nuclear translocation, and increased ROS levels and apoptotic cells	Redox Biol. 2022 Oct;56:102468.
human dental pulp stem cells	10 µM	7 days	LY294002 attenuated the responsiveness of 10−6 M insulin to IIS/PI3K/AKT/mTOR pathway axis, suppressing the promoting effect of insulin on cell proliferation, osteogenic differentiation and bone formation.	Stem Cell Res Ther. 2024 Jul 29;15(1):227.
PC-9R cells	25 μM		Inhibited the PI3K/AKT pathway and restored sensitivity to gefitinib in PC-9R cells	J Cancer. 2022 Mar 21;13(6):1837-1847.
BMDMs	0.5 μM	2 h	Inhibited PI3K/Akt/Nrf2 signaling pathway and increased NLRP3/Caspase-1/GSDMD protein expression	Phytomedicine. 2023 Jun;114:154753.
A549 cells	10μM	1 h	Inhibited PI3K/AKT signaling pathway, alleviated TGF-β1-induced epithelial-mesenchymal transition (EMT)	Front Pharmacol. 2022 Mar 9;13:829673.
Huh7-SR cells	5 µM	1 h	Inhibited PI3K/Akt pathway, reduced Nrf2 nuclear translocation, and increased ferroptosis level	Front Oncol. 2022 Mar 22;12:852095.
HepG2-SR cells	5 µM	1 h	Inhibited PI3K/Akt pathway, reduced Nrf2 nuclear translocation, and increased ferroptosis level	Front Oncol. 2022 Mar 22;12:852095.
Mouse primary hepatocytes	10 μM	1.5 h	To evaluate the relationship between PI3K/AKT pathway and ferroptosis, LY294002 pretreatment exacerbated ferroptosis	Transplantation. 2024 Nov 1;108(11):e357-e369.

Species Mice C57BL/6 mice BALB/c nude mice C57BL/6 mice Mice NOD mice NOD-SCID mice C57 mice	Animal Model Experimental autoimmune hepatitis model Myocardial infarction model (LAD ligation) PC-9R cell xenograft model Acute lung injury model Bleomycin-induced pulmonary fibrosis model Diabetes model Subcutaneous tumor model Liver warm ischemia/reperfusion model	Administration	Dosage	Frequency	Description	References
Mice	Experimental autoimmune hepatitis model	Intraperitoneal injection	30 mg/kg	Pretreatment 30 minutes before	Inhibit PI3K signaling pathway and reduce FGF4's regulatory effect on M1 macrophages	J Transl Med. 2024 Aug 2;22(1):717.
C57BL/6 mice	Myocardial infarction model (LAD ligation)	Intraperitoneal injection	2.5 mg/kg	From LAD operation to 7 days post-operation	Inhibited PI3K α/AKT signaling, abolished FGF7-mediated regulation of Nrf2 and HXK2, and exacerbated myocardial oxidative stress and apoptosis	Redox Biol. 2022 Oct;56:102468.
BALB/c nude mice	PC-9R cell xenograft model	Intraperitoneal injection	2.5 mg/kg	Every three days for 12 days	LY294002 significantly reduced tumor volume and enhanced the anti-tumor effect of gefitinib	J Cancer. 2022 Mar 21;13(6):1837-1847.
C57BL/6 mice	Acute lung injury model	Injection	20 mg/kg	24 hours	Inhibited PI3K/Akt/Nrf2 signaling pathway and increased NLRP3/Caspase-1/GSDMD protein expression	Phytomedicine. 2023 Jun;114:154753.
Mice	Bleomycin-induced pulmonary fibrosis model	Intraperitoneal injection	25 mg/kg	Every other day for 21 days	Inhibited PI3K/AKT signaling pathway, alleviated bleomycin-induced pulmonary fibrosis and EMT	Front Pharmacol. 2022 Mar 9;13:829673.
NOD mice	Diabetes model	Intraperitoneal injection	75 mg/kg	Daily for 3 days	Inhibition of PI3K signaling pathway to observe its effect on CD4+ T cell migration	J Immunol. 2016 Nov 1;197(9):3504-3511
NOD-SCID mice	Subcutaneous tumor model	Intraperitoneal injection	25 mg/kg	Twice a week for 4 weeks	Inhibited PI3K/Akt pathway, slowed growth of FNDC5-overexpressing HCC cells, and increased ferroptosis level	Front Oncol. 2022 Mar 22;12:852095.
C57 mice	Liver warm ischemia/reperfusion model	Intraperitoneal injection	10 mg/kg	Single dose 36 h before liver ischemia followed by 6 h reperfusion	To assess the role of PI3K/AKT pathway in hepatic I/R injury, LY294002 pretreatment abolished the protective effect of rmGas6 and exacerbated ferroptosis	Transplantation. 2024 Nov 1;108(11):e357-e369.

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 <<

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	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

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]

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

CAS号	154447-36-6
分子式	C₁₉H₁₇NO₃
分子量	307.34
SMILES Code	O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC=C4
MDL No.	MFCD00270881

别名	SF 1101; NSC 697286
运输	蓝冰
InChI Key	CZQHHVNHHHRRDU-UHFFFAOYSA-N
Pubchem ID	3973

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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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