PI3K

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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  1. PP121

    Catalog No. A11207
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    PI3K Inhibitor
    PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). Learn More
  2. VS-5584

    Catalog No. A12480
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    PI3K/mTOR inhibitor
    VS-5584 is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Learn More
  3. HS-173

    Catalog No. A13021
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    PI3K Inhibitor
    HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. Learn More
  4. Panulisib (P7170, AK151761)

    Catalog No. A14379
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    PI3K inhibitor
    Panulisib is a potent and selective imidazoquinoline based PI3K inhibitor with potential anticancer activity. Learn More
  5. AZD8186

    Catalog No. A14164
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    PI3K inhibitor
    AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity. Learn More
  6. CAL-130

    Catalog No. A15030
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    PI3K inhibitor
    CAL-130 is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kδ/γ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Learn More
  7. CAL-130 Hydrochloride

    Catalog No. A15031
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    PI3K inhibitor
    CAL-130 Hydrochloride is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kδ/γ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Learn More
  8. LY 303511

    Catalog No. A15147
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    PI3K inhibitor
    LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. Learn More
  9. NVP-BKM120 Hydrochloride

    Catalog No. A15195
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    PI3K Inhibitor‎
    NVP-BKM120 Hydrochloride is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNA-PK, with little activity to PI4Kβ. Learn More
  10. PI-103 Hydrochloride

    Catalog No. A15212
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    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. Learn More
  11. XL-147 (Pilaralisib)

    Catalog No. A15283
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    PI3K Inhibitor
    XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases. Learn More
  12. AZD8186

    Catalog No. A15759
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    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). Learn More
  13. Acalisib (GS-9820)

    Catalog No. A14441
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    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. Learn More
  14. AMG319

    Catalog No. A15901
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    PI3Kδ inhibitor
    AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. Learn More
  15. PF-4989216

    Catalog No. A12889
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    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 p110α, p110β, p110γ, p110δ, and VPS34, respectively. Learn More
  16. PQR309 (Bimiralisib)

    Catalog No. A15992
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    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. Learn More
  17. GNE-317

    Catalog No. A13992
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    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. Learn More
  18. LY3023414

    Catalog No. A16126
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    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). Learn More
  19. ON 146040

    Catalog No. A16266
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    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. Learn More
  20. PI4KIIIbeta-IN-10

    Catalog No. A16269
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    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). Learn More
  21. PI4KIIIbeta-IN-9

    Catalog No. A16270
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    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. Learn More
  22. ETP-46321

    Catalog No. A16271
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    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. Learn More
  23. GDC-0084

    Catalog No. A16272
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    PI3K inhibitor
    GDC-0084 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Learn More
  24. NVP-QAV-572

    Catalog No. A16273
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    PI3K inhibitor
    NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM. Learn More
  25. PI3K-alpha inhibitor 1

    Catalog No. A16274
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    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) . Learn More
  26. PI3K-gamma inhibitor 1

    Catalog No. A16275
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    PI3Kγ inhibitor
    PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor. Learn More
  27. SAR245409 (XL765, Voxtalisib)

    Catalog No. A16276
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    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. Learn More
  28. TGR-1202 (Umbralisib)

    Catalog No. A16277
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    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. Learn More
  29. TGR-1202 hydrochloride (Umbralisib HCl)

    Catalog No. A16278
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    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. Learn More
  30. IPI-3063

    Catalog No. A16800
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    selective p110δ inhibitor
    IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5±1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. Learn More
  31. 2-D08

    Catalog No. A16852
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    SUMO inhibitor
    2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays. Learn More
  32. 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. Learn More
  33. 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. Learn More
  34. 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). Learn More
  35. SAR405

    Catalog No. A21345
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    PI3KC3 isoform Vps34 inhibitor
    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PI3KC3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). Learn More
  36. 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. Learn More
  37. LY294002

    Catalog No. A10547
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    PI3K Inhibitor
    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor. Learn More
  38. BEZ235 (NVP-BEZ235, Dactolisib)

    Catalog No. A10133
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    PI3K/mTOR Inhibitor
    BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Learn More
  39. BKM120 (NVP-BKM120, Buparlisib)

    Catalog No. A11016
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    PI3K Inhibitor‎
    BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor. Learn More
  40. GDC-0941 (Pictilisib)

    Catalog No. A10421
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    PI3K inhibitor
    GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively. Learn More
  41. AZD6482

    Catalog No. A10112
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    PI3K inhibitor
    AZD6482 is a PI3Kbeta inhibitor (IC50=0.021M) used in antithrombotic therapy. Learn More
  42. ZSTK474

    Catalog No. A11014
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    PI3K inhibitor
    ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Learn More
  43. IC-87114

    Catalog No. A10463
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    PI3K Inhibitor
    IC-87114 was the first isoform-selective PI3K inhibitor :p110M-NM-4(IC50 = 0.13 M-BM-5M) vs. p110M-NM-1(IC50 = 200 M-BM-5M), p110M-NM-2(IC50 = 16 M-BM-5M) and p110M-NM-3(IC50 = 61 M-BM-5M). Learn More
  44. PI-103

    Catalog No. A10726
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    PI3K Inhibitor
    PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR. Learn More
  45. XL147 analogue

    Catalog No. A10995
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    PI3K Inhibitor
    XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity. Learn More
  46. CAL-101 (GS-1101, Idelalisib)

    Catalog No. A10172
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    PI3K inhibitor
    CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells. Learn More
  47. AS-605240

    Catalog No. A10088
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    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. Learn More
  48. GSK1059615

    Catalog No. A10438
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    mTOR/PI3K Inhibitor
    GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM). Learn More
  49. TGX-221

    Catalog No. A10923
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    PI3K Inhibitor
    TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β. Learn More
  50. TG100-115

    Catalog No. A10922
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    PI3K Inhibitor
    TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively). Learn More

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