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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Set Descending Direction
Catalog No. Product Name Application Product Information
A11151 SALE

3-Methyladenine

Autophagy/PI3K Inhibitor
3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
A11202

A66

PI3K inhibitor
The S-enantiomer of A66 is a potent inhibitor of the p110alpha isoform of PI 3-kinase (PIK3CA).
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.
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.
A11099 SALE

AS-252424

PI3K inhibitor
AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000, and 20,000 nM respectively.
A11197 SALE

AS-604850

PI3K Inhibitor

AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.

A10088

AS-605240

PI3K Inhibitor
AS-605240 is an orally active inhibitor of PI3-kinase γ that inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.
A10112 SALE

AZD6482

PI3K inhibitor
AZD6482 is a PI3Kbeta inhibitor (IC50=0.021M) used in antithrombotic therapy.
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).
A14164 SALE

AZD8186

PI3K inhibitor
AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.
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).
A11766 SALE

BAY 80-6946 (Copanlisib)

PI3K inhibitor
BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
A10133 SALE

BEZ235 (NVP-BEZ235, Dactolisib)

PI3K/mTOR Inhibitor
BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
A11016 SALE

BKM120 (NVP-BKM120, Buparlisib)

PI3K Inhibitor‎
BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.
A11328 SALE

BYL719 (Alpelisib)

PI3K Inhibitor
BLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
A10172 SALE

CAL-101 (GS-1101, Idelalisib)

PI3K inhibitor
CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.
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).
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).
A11196 SALE

CAY10505

PI3K inhibitor

CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively).

A11169 SALE

CH5132799

PI3K inhibitor

CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM).

A13879

CNX-1351

PI3Kα inhibitor
A11153 SALE

CUDC-907

HDAC inhibitor
CUDC-907 is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.
A11363 SALE

CZC24832

PI3K inhibitor
CZC24832 is a selective inhibitor of PI 3-Kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay).
A11198

D-106669

PI3K Inhibitor

D-106669 is a highly potent and selective PI3K inhibitor, (PI3Kα IC50 <10 nM, >3 log selectivity against tyrosine or serine/threonine kinases, except ERK1 and 2).

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.

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