PI3K

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PI3K	p110α	p110β	p110δ	p110γ	C2α	C2β	Vps34	Other Targets
A10133	Dactolisib (BEZ235, NVP-BEZ235)		****	**	***	***				mTOR (p70S6K),ATR
A10421	Pictilisib (GDC-0941)		****	**	****	**		*		mTOR
A10547	LY294002		*	*	*
A10172	Idelalisib (CAL-101, GS-1101)		*	*	****	**			*	DNA-PK
A11016	Buparlisib (BKM120, NVP-BKM120)		**	*	**	*			*	mTOR
A10726	PI-103		****	****	****	***				DNA-PK,mTOR
A10923	TGX-221		*	****	**
A10463	IC-87114			*	**	*
A11161	Wortmannin	****								DNA-PK,ATM,MLCK
A10995	XL147 analogue		***	**	***	***
A11014	ZSTK474	***	***	***	****	**
A11328	Alpelisib (BYL719)		****
A10088	AS-605240		**	*	*	***
A10729	PIK-75 HCl		***		*	**				DNA-PK
A11151	3-Methyladenine (3-MA)					*			*
A11202	A66		***			*		*		PI4Kβ
A10731	PIK-93		***	*	**	***	*	**	*	PI4KIIIβ,DNA-PK,ATM
A11035	Omipalisib (GSK2126458, GSK458)		****	****	****	****				mTORC1,mTORC2
A10730	PIK-90		***	*	**	***
A11024	PF-04691502		****	****	****	****				P-Akt (S473),P-Akt (T308),mTOR
A10112	AZD6482		*	***	**	*				DNA-PK
A11023	Apitolisib (GDC-0980, RG7422)		****	***	***	***				mTOR
A10438	GSK1059615		****	****	****	****				mTOR
A12422	Duvelisib (IPI-145, INK1197)		***	****	****	****
A11079	Gedatolisib (PF-05212384, PKI-587)		****			****				mTOR
A10922	TG100-115		*	*	**	**
A11099	AS-252424		*			***				Casein Kinase 2
A11162	BGT226 (NVP-BGT226)		****	**		***				mTOR
A11153	CUDC-907		***	**	***	*				HDAC1,HDAC3,HDAC10
A10728	PIK-294			*	***	**
A11197	AS-604850		*			**
A11766	Copanlisib (BAY 80-6946)		****	****	****	***
A11064	YM201636		*							PIKfyve
A11169	CH5132799		***	**	*	***
A10727	PIK-293		*	*	**	*
A11089	PKI-402		****	***	***	***				mTOR
A11956	TG100713		**	**	***	**
A12480	VS-5584 (SB2343)		****	***	****	****				mTOR
A12831	Taselisib (GDC 0032)		****	***	****	****		*	*
A11363	CZC24832			*	*	***
A16332	IPI-549		*	*	*	***
A16277	TGR-1202				***
A16272	GDC-0084		****	**	****	***				mTOR
A16352	AZD8835		***	*	****	**
A15868	PIK-III		*	*	*				***
A15874	VPS34-IN1								***
A16276	Voxtalisib (XL765, SAR245409)		***	**	**	***				DNA-PK,mTOR
A15901	AMG319		*	*	***	*
A15759	AZD8186		***	****	***	*
A12889	PF-4989216		****	**	****	**
A15283	Pilaralisib (XL147)		**	***	***	***
A14338	PI-3065		*	*	***	*
A13021	HS-173		****
A10766	Quercetin			*	*	*				PKC,Src,Sirtuin
A11784	GSK2636771
A11196	CAY10505
A16126	LY3023414									DNA-PK,mTOR kinase
A13992	GNE-317
A14441	Acalisib (GS-9820)
A16273	NVP-QAV-572
A16266	ON 146040		***		***
A15992	PQR309
A15529	MLN1117 (Serabelisib)		***
A15030	CAL-130
A14379	Panulisib (P7170, AK151761)									ALK1, mTOR, DNA-PK
A13879	CNX-1351		****
A11198	D-106669		****
A11261	PX-866 (Sonolisib)		****	*	****	***
A11511	NVP-BAG956		***	*	***	**				PDK1
A12935	PF-04979064	****	****		****	****				mTOR
A13328	ETP-46464		*							mTOR, DNA-PK, ATR, ATM
A14432	GNE-493		****	***	***	***				mTOR

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Acalisib (GS-9820)

Catalog No. A14441
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PI3Kδ 抑制剂

Acalisib (GS-9820)是IA类磷酸肌醇3激酶（PI3K）的110 kDa催化亚基的β和δ异构体的抑制剂，具有潜在的免疫调节和抗肿瘤活性。了解更多

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AMG319

Catalog No. A15901
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PI3Kδ 抑制剂

AMG319是一种有效的选择性PI3Kδ抑制剂，IC50为18 nM，选择性是其他PI3K的47倍以上。了解更多

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PF-4989216

Catalog No. A12889
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PI3K 抑制剂

PF-4989216是一种有效的选择性PI3K抑制剂，对p110α，p110β，p110γ，p110δ和VPS34的IC50分别为2 nM，142 nM，65 nM，1 nM和110 nM。了解更多

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PQR309 (Bimiralisib)

Catalog No. A15992
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PI3K 抑制剂

PQR309是磷酸肌醇3激酶（PI3K）的口服生物利用泛抑制剂，是雷帕霉素哺乳动物靶标（mTOR）的抑制剂，具有潜在的抗肿瘤活性。了解更多

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GNE-317

Catalog No. A13992
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PI3K 抑制剂

GNE-317是一种有效的PI3K抑制剂，可以穿过血液的脑屏障。显示了完整BBB小鼠大脑中PI3K途径的有效抑制。了解更多

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LY3023414

Catalog No. A16126
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PI3K/mTOR Dual 抑制剂

LY3023414是从专利WO/2012097039A1（化合物实施例1）中提取的I类PI3K同种型，mTOR和DNA-PK的口服ATP竞争性抑制剂，对Akt1（pT308）的IC50为64.9 nM，42.1 nM，10.6 nM和19.1 nM。），Akt1（pS473），P70S6（pT389），S6RP（pS240/242）。了解更多

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- Zou Y, .et al. Targeting PI3K-AKT-mTOR by LY3023414 inhibits human skin squamous cell carcinoma cell growth in vitro and in vivo, Biochem Biophys Res Commun, 2017, Aug 19;490(2):385-392 PMID: 28623128
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ON 146040

Catalog No. A16266
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dual PI3K and BCR-ABL 抑制剂

ON 146040是第一个靶向STAT3和STAT5途径的PI3K和BCR-ABL双重抑制剂；抑制PI3Kα/δ同工型，IC50为14/20 nM。了解更多

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PI4KIIIbeta-IN-10

Catalog No. A16269
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PI4KIIIβ 抑制剂

PI4KIIIbeta-IN-10是目前报道的最有效的PI4KIIIbeta抑制剂，对PI4KIIIbeta相关的脂质激酶的脱靶抑制作用很小（IC50 = 3.6 nM）。了解更多

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PI4KIIIbeta-IN-9

Catalog No. A16270
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PI4KIIIβ 抑制剂

PI4KIIIbeta-IN-9是一种有效的PI4KIIIbeta抑制剂（IC50为7 nM），选择性是PI3Kgamma的140倍以上，选择性是PI3Kδ的20倍以上，并且在浓度高达20 uM时，对vps34没有抑制作用。了解更多

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ETP-46321

Catalog No. A16271
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PI3K α/δ 抑制剂

ETP-46321是一种有效且口服可生物利用的PI3Kα/δ抑制剂，口服后具有有效的生化和细胞活性，并具有良好的药代动力学特性（PK）。了解更多

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NVP-QAV-572

Catalog No. A16273
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PI3K 抑制剂

NVP-QAV-572是一种有效的PI3K kianse抑制剂，IC50为10 nM。了解更多

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PI3K-alpha inhibitor 1

Catalog No. A16274
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PI3Kα 抑制剂

PI3K-alpha inhibitor 1 是从专利US/20120088764A1中提取的PI3Kα抑制剂，化合物243，IC50 <0.1uM，PI3Kα抑制剂1还抑制HDAC（0.1uM≤IC50≤1uM）。了解更多

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PI3K-gamma inhibitor 1

Catalog No. A16275
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PI3Kγ 抑制剂

PI3K-gamma inhibitor 1 是有效的PI3Kγ抑制剂。了解更多

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SAR245409 (XL765, Voxtalisib)

Catalog No. A16276
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PI3K/mTOR dual 抑制剂

SAR245409 (XL765,Voxtalisib)是PI3K/mTOR双激酶抑制剂XL765是口服生物可利用的小分子，靶向PI3K/mTOR信号途径中的磷脂酰肌醇3激酶（PI3K）和雷帕霉素（mTOR）激酶的哺乳动物靶标，具有潜在的抗肿瘤活性。了解更多

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TGR-1202 (Umbralisib)

Catalog No. A16277
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PI3Kδ 抑制剂

TGR-1202是口服的下一代PI3Kδ抑制剂，在基于酶和细胞的测定中抑制PI3Kδ活性，IC50和EC50值分别为22.2和24.3 nM。了解更多

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TGR-1202 hydrochloride (Umbralisib HCl)

Catalog No. A16278
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PI3Kδ 抑制剂

TGR-1202 hydrochloride是一种口服的下一代PI3Kδ抑制剂，在基于酶和细胞的测定中抑制PI3Kδ活性，IC50和EC50值分别为22.2和24.3 nM。了解更多

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AZD8835

Catalog No. A16352
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PI3Kα/PI3Kδ 抑制剂

AZD8835是一种有效的选择性PI3Kα和PI3Kδ抑制剂，IC50为5.7 nM和6.2 nM，对PI3Kβ（IC50 431 nM）和PI3Kγ（IC50 90 nM）具有选择性。了解更多

Product Citations (1)

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- James T. Lynch, etc. Identification of differential PI3K pathway target dependencies in T-cell acute lymphoblastic leukemia through a large cancer cell panel screen. Oncotarget. 2016 Apr 19; 7(16): 22128–22139.
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IPI-3063

Catalog No. A16800
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selective p110δ 抑制剂

IPI-3063是一种有效的选择性p110δ抑制剂，生化IC50为2.5±1.2 nM，其他I类PI3K亚型（p110α，p110β，p110γ）的IC50值至少高400倍。了解更多

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2-D08

Catalog No. A16852
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SUMO 抑制剂

2-D08是细胞可渗透的，机械上独特的蛋白质sumoylation抑制剂。在生化测定中，它也抑制Axl，IRAK4，ROS1，MLK4，GSK3β，RET，KDR和PI3Kα，IC50值分别为0.49、3.9、5.3、9.8、11、11、17和35 nM。了解更多

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IITZ-01

Catalog No. A20192
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Lysosomotropic autophagy inhibitor

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ. 了解更多

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alpha-Bisabolol

Catalog No. A18691
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alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells. 了解更多

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OSU-T315

Catalog No. A20870
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ILK inhibitor

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). 了解更多

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SAR405

Catalog No. A21345
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PIK3C3 isoform Vps34 inhibitor

SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). 了解更多

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Rigosertib sodium

Catalog No. A21824
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multi-kinase inhibitor

Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. 了解更多

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