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PI3K

Inhibitory Selectivity
Catalog No.Inhibitor Name PI3K p110α p110β p110δ p110γC2α C2β Vps34 Other Targets
A10133Dactolisib (BEZ235, NVP-BEZ235)
****
**
***
***
mTOR (p70S6K),ATR
A10421Pictilisib (GDC-0941)
****
**
****
**
*
mTOR
A10547LY294002
*
*
*
A10172Idelalisib (CAL-101, GS-1101)
*
*
****
**
*
DNA-PK
A11016Buparlisib (BKM120, NVP-BKM120)
**
*
**
*
*
mTOR
A10726PI-103
****
****
****
***
DNA-PK,mTOR
A10923TGX-221
*
****
**
A10463IC-87114
*
**
*
A11161Wortmannin
****
DNA-PK,ATM,MLCK
A10995XL147 analogue
***
**
***
***
A11014ZSTK474
***
***
***
****
**
A11328Alpelisib (BYL719)
****
A10088AS-605240
**
*
*
***
A10729PIK-75 HCl
***
*
**
DNA-PK
A111513-Methyladenine (3-MA)
*
*
A11202A66
***
*
*
PI4Kβ
A10731PIK-93
***
*
**
***
*
**
*
PI4KIIIβ,DNA-PK,ATM
A11035Omipalisib (GSK2126458, GSK458)
****
****
****
****
mTORC1,mTORC2
A10730PIK-90
***
*
**
***
A11024PF-04691502
****
****
****
****
P-Akt (S473),P-Akt (T308),mTOR
A10112AZD6482
*
***
**
*
DNA-PK
A11023Apitolisib (GDC-0980, RG7422)
****
***
***
***
mTOR
A10438GSK1059615
****
****
****
****
mTOR
A12422Duvelisib (IPI-145, INK1197)
***
****
****
****
A11079Gedatolisib (PF-05212384, PKI-587)
****
****
mTOR
A10922TG100-115
*
*
**
**
A11099AS-252424
*
***
Casein Kinase 2
A11162BGT226 (NVP-BGT226)
****
**
***
mTOR
A11153CUDC-907
***
**
***
*
HDAC1,HDAC3,HDAC10
A10728PIK-294
*
***
**
A11197AS-604850
*
**
A11766Copanlisib (BAY 80-6946)
****
****
****
***
A11064YM201636
*
PIKfyve
A11169CH5132799
***
**
*
***
A10727PIK-293
*
*
**
*
A11089PKI-402
****
***
***
***
mTOR
A11956TG100713
**
**
***
**
A12480VS-5584 (SB2343)
****
***
****
****
mTOR
A12831Taselisib (GDC 0032)
****
***
****
****
*
*
A11363CZC24832
*
*
***
A16332IPI-549
*
*
*
***
A16277TGR-1202
***
A16272GDC-0084
****
**
****
***
mTOR
A16352AZD8835
***
*
****
**
A15868PIK-III
*
*
*
***
A15874VPS34-IN1
***
A16276Voxtalisib (XL765, SAR245409)
***
**
**
***
DNA-PK,mTOR
A15901AMG319
*
*
***
*
A15759AZD8186
***
****
***
*
A12889PF-4989216
****
**
****
**
A15283Pilaralisib (XL147)
**
***
***
***
A14338PI-3065
*
*
***
*
A13021HS-173
****
A10766Quercetin
*
*
*
PKC,Src,Sirtuin
A11784GSK2636771
A11196CAY10505
A16126LY3023414
DNA-PK,mTOR kinase
A13992GNE-317
A14441Acalisib (GS-9820)
A16273NVP-QAV-572
A16266ON 146040
***
***
A15992PQR309
A15529MLN1117 (Serabelisib)
***
A15030CAL-130
A14379Panulisib (P7170, AK151761)
ALK1, mTOR, DNA-PK
A13879 CNX-1351
****
A11198D-106669
****
A11261PX-866 (Sonolisib)
****
*
****
***
A11511NVP-BAG956
***
*
***
**
PDK1
A12935PF-04979064
****
****
****
****
mTOR
A13328ETP-46464
*
mTOR, DNA-PK, ATR, ATM
A14432GNE-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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Catalog No. Product Name Application Product Information
A13021 SALE

HS-173

PI3K Inhibitor
HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis.
A15147

LY 303511

PI3K inhibitor
LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K.
A12889

PF-4989216

PI3K inhibitor
PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110??, p110??, p110??, p110??, and VPS34, respectively.
A15901

AMG319

PI3Kδ inhibitor
AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
A14441

Acalisib (GS-9820)

PI3Kδ Inhibitor
Acalisib is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities.
A15759 SALE

AZD8186

PI3K inhibitor
AZD8186 is an isoform-specific small-molecule PI3K inhibitor, potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
A15283

XL-147 (Pilaralisib)

PI3K Inhibitor
XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases.
A15212

PI-103 Hydrochloride

PI3K Inhibitor
PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
A15195

NVP-BKM120 Hydrochloride

PI3K Inhibitor‎
NVP-BKM120 Hydrochloride is a selective PI3K inhibitor of p110??/??/??/?? with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4K??.
A15031

CAL-130 Hydrochloride

PI3K inhibitor
CAL-130 Hydrochloride is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3K??/?? as therapy for T cell acute lymphoblastic leukemia (T-ALL).
A15030

CAL-130

PI3K inhibitor
CAL-130 is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3K??/?? as therapy for T cell acute lymphoblastic leukemia (T-ALL).
A14164 SALE

AZD8186

PI3K inhibitor
AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.
A14379

Panulisib (P7170, AK151761)

PI3K inhibitor
Panulisib is a potent and selective imidazoquinoline based PI3K inhibitor with potential anticancer activity.
A12480 SALE

VS-5584

PI3K/mTOR inhibitor
VS-5584 is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
A15992

PQR309

PI3K inhibitor
PQR309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
A13992

GNE-317

PI3K inhibitor
GNE-317 is a potent PI3K inhibitor that can cross the Blood brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.
A16126

LY3023414

PI3K/mTOR Dual Inhibitor
LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).
A16278

TGR-1202 hydrochloride

PI3Kδ inhibitor
TGR-1202 hydrochloride is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
A16277

TGR-1202

PI3Kδ inhibitor
TGR-1202 is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
A16276

SAR245409 (XL765, Voxtalisib)

PI3K/mTOR dual inhibitor
SAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity.
A16275

PI3K-gamma inhibitor 1

PI3Kγ inhibitor
PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor.
A16270

PI4KIIIbeta-IN-9

PI4KIIIβ inhibitor
PI4KIIIbeta-IN-9 is a potent PI4KIIIbeta inhibitor (IC50 of 7 nM) and is >140-fold selective over PI3Kgamma and >20-fold selective over PI3Kδ, and shows no inhibition of vps34 at concentrations up to 20 uM.
A16274

PI3K-alpha inhibitor 1

PI3Kα inhibitor
PI3Kα inhibitor 1 is a PI3Kα inhibitor extracted from patent US/20120088764A1, compound 243, has an IC50 < 0.1 uM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 uM ≤ IC50 ≤ 1 uM) .
A16273

NVP-QAV-572

PI3K inhibitor
NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM.
A16272

GDC-0084

PI3K inhibitor
GDC-0084 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
A16271

ETP-46321

PI3K α/δ inhibitor
ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing.
A16269

PI4KIIIbeta-IN-10

PI4KIIIβ inhibitor
PI4KIIIbeta-IN-10 is the most potent PI4KIIIbeta inhibitor currently reported, with very minor off-target inhibition of PI4KIIIbeta related lipid kinases (IC50 = 3.6 nM).
A16266

ON 146040

dual PI3K and BCR-ABL inhibitor
ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.
A14138

Miltefosine

PI3K/Akt inhibitor
Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa
A14114

GNE 477

PI3K/mTOR inhibitor
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
A12704

SF1126

Pan PI3K inhibitor
SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities.
A13879

CNX-1351

PI3Kα inhibitor
A12831 SALE

GDC-0032 (Taselisib)

PI3K inhibitor
GDC-0032 is a potent, next-generation PI3 inhibitor targeting PI3 alpha.
A13328

ETP-46464

ATR inhibitor
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
A12935

PF-04979064

PI3K/mTOR Dual Inhibitor
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor.
A14109

PI3k-delta inhibitor 1

PI3Kδ inhibitor
N/A
A16332

IPI-549

PI3Kγ Inhibitor
IPI-549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM.
A15529 SALE

MLN1117 (Serabelisib)

p110α inhibitor
MLN1117, also known as INK1117 and TAK-117, is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.
A10438 SALE

GSK1059615

mTOR/PI3K Inhibitor
GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).
A15874

VPS34-IN1

Vps34 Inhibitor
Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
A16352

AZD8835

PI3Kα/PI3Kδ inhibitor
AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50 of 5.7 nM and 6.2 nM, with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM).
A15430

PI4KIII beta inhibitor 3

PI4KIII beta inhibitor
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIII beta inhibitor with IC50 of 5.7 nM.
A15868

PIK-III

Autophagy Inhibitor
PIK-III is a selective inhibitor of ?VPS34 enzymatic activity.
A14432

GNE-493

Dual Pan PI3k/mTOR inhibitor
GNE-493 is potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor with potential anticancer activity.
A14338 SALE

PI-3065

p110δ inhibitor
PI-3065 is a small molecule and selective inhibitor of p110δ kinase with an Ki value of 1.5nM and IC50 value of 5nM
A12422 SALE

IPI-145 (Duvelisib, INK1197)

PI3K-δ/PI3K-γ inhibitor
IPI-145, also known as INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.
A10547 SALE

LY294002

PI3K Inhibitor
LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
A10922 SALE

TG100-115

PI3K Inhibitor
TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).
A11023 SALE

GDC-0980 (Apitolisib, RG7422)

mTOR/PI3K Inhibitor
GDC-0980 (RG7422) is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms, respectively.
A11024 SALE

PF-04691502

PI3K/mTOR Inhibitor
PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.

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