1. Signaling Pathways
  2. PI3K/Akt/mTOR
  3. PI3K
  4. PI3Kα Inhibitors

PI3Kα Inhibitors

PI3Kα

PI3Kβ

PI3Kγ

PI3Kδ

PI3KC2α

PI3KC2β

PI3KC2γ

Vps34

PI3K

PI3KC3

p120γ

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Sorry. There is currently no product that acts on isoform PI3Kα together.

Please try each isoform separately.

PI3Kα Specific Inhibitors
Product Name PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3KC3 p120γ PI3Kα Selectivity Purity
Alpelisib
p110α, IC50: 5 nM
p110α-H1047R, IC50: 4 nM
p110α-E545K, IC50: 4 nM
p110β, IC50: 1200 nM
p110γ, IC50: 250 nM
p110δ, IC50: 290 nM
            Selective Inhibitor 99.90%
YM-201636
p110α, IC50: 3.3 μM
                  Selective Inhibitor 98.22%
HS-173
PI3Kα, IC50: 0.8 nM
                  Selective Inhibitor 99.32%
Serabelisib
p110α, IC50: 15 nM
p110β, IC50: 4500 nM
p110γ, IC50: 1900 nM
p110δ, IC50: 13900 nM
            Selective Inhibitor 99.66%
PIK-75
p110α, IC50: 5.8 nM
p110β, IC50: 1.3 μM
p110γ, IC50: 76 nM
p110δ, IC50: 510 nM
PI3KC2α, IC50: 10 μM
PI3KC2β, IC50: 1 μM
 
hsVPS34, IC50: 2.6 μM
    Selective Inhibitor 99.91%
GDC-0326
PI3Kα, Ki: 0.2 nM
PI3Kβ, Ki: 26.6 nM
PI3Kγ, Ki: 10.2 nM
PI3Kδ, Ki: 4 nM
            Selective Inhibitor 99.31%
PF-4989216
PI3Kα, Ki: 0.6 nM
                  Selective Inhibitor 99.43%
A66
p110α, IC50: 32 nM
p110α E545K, IC50: 30 nM
p110α H1047R, IC50: 43 nM
 
p110γ, IC50: 3480 nM
   
PI3K-C2β, IC50: 462 nM
        Selective Inhibitor 99.26%
Pilaralisib analogue
PI3K-alpha
                  Selective Inhibitor 96.75%
BEBT-908
PI3Kα, IC50: 0.1 μM
                  Selective Inhibitor >98.0%
KU-0060648
PI3Kα, IC50: 4 nM
PI3Kβ, IC50: 0.5 nM
PI3Kγ, IC50: 0.594 μM
PI3Kδ, IC50: 0.1 nM
            Selective Inhibitor
PI3Kα/mTOR-IN-1
PI3Kα, Ki: 12.5 nM
PI3Kα, IC50: 7 nM (Cell Assay)
                  Selective Inhibitor
LY294002
p110α, IC50: 0.5 μM
p110β, IC50: 0.97 μM
 
p110δ, IC50: 0.57 μM
            Pan Inhibitor 99.95%
Copanlisib
PI3Kα, IC50: 0.5 nM
PI3Kβ, IC50: 3.7 nM
PI3Kγ, IC50: 6.4 nM
PI3Kδ, IC50: 0.7 nM
            Pan Inhibitor 98.91%
BGT226
PI3Kα, IC50: 4 nM
PI3Kβ, IC50: 63 nM
PI3Kγ, IC50: 38 nM
              Pan Inhibitor
Buparlisib
p110α, IC50: 52 nM
p110α-H1047R, IC50: 58 nM
p110α-E545K, IC50: 99 nM
p110β, IC50: 166 nM
p110γ, IC50: 262 nM
p110δ, IC50: 116 nM
     
Vps34, IC50: 2.4 μM
    Pan Inhibitor 99.90%
Idelalisib
p110α, IC50: 820 nM
p110β, IC50: 565 nM
p110γ, IC50: 89 nM
p110δ, IC50: 2.5 nM
     
hVps34, IC50: 978 nM
    Pan Inhibitor 99.98%
IPI549
PI3Kα, IC50: 3.2 μM
PI3Kβ, IC50: 3.5 μM
PI3Kγ, IC50: 16 nM
              Pan Inhibitor 99.34%
Dactolisib
p110α, IC50: 4 nM
p110α-H1047R, IC50: 4.6 nM
p110α-E545K, IC50: 5.7 nM
p110β, IC50: 75 nM
p110γ, IC50: 5 nM
p110δ, IC50: 7 nM
            Pan Inhibitor 99.13%
Pictilisib
p110α, IC50: 3 nM
p110α-H1047R, IC50: 3 nM
p110α-E545K, IC50: 3 nM
p110β, IC50: 33 nM
p110γ, IC50: 75 nM
p110δ, IC50: 3 nM
            Pan Inhibitor 99.62%
LY3023414
PI3Kα, IC50: 6.07 nM
PI3Kβ, IC50: 77.6 nM
PI3Kγ, IC50: 23.8 nM
PI3Kδ, IC50: 38 nM
            Pan Inhibitor 99.77%
Fimepinostat
PI3Kα, IC50: 19 nM
PI3Kβ, IC50: 54 nM
PI3Kγ, IC50: 311 nM
PI3Kδ, IC50: 39 nM
            Pan Inhibitor 99.95%
Duvelisib
p110α, IC50: 1602 nM
p110β, IC50: 85 nM
p110γ, IC50: 27.4 nM
p110δ, IC50: 2.5 nM
            Pan Inhibitor 99.91%
PI-103
p110α, IC50: 8 nM
p110β, IC50: 88 nM
p110γ, IC50: 150 nM
p110δ, IC50: 48 nM
PI3KC2α, IC50: 1 μM
PI3KC2β, IC50: 26 nM
 
hsVPS34, IC50: 2.3 μM
    Pan Inhibitor 99.86%
PF-04691502
PI3Kα, Ki: 1.8 nM
PI3Kβ, Ki: 2.1 nM
PI3Kγ, Ki: 1.9 nM
PI3Kδ, Ki: 1.6 nM
            Pan Inhibitor 99.49%
Omipalisib
p110α, Ki: 0.019 nM
p110α-H1047R, Ki: 0.009 nM
p110α-E545K, Ki: 0.008 nM
p110α-E542K, Ki: 0.008 nM
p110β, Ki: 0.13 nM
p110γ, Ki: 0.06 nM
p110δ, Ki: 0.024 nM
            Pan Inhibitor 99.31%
Taselisib
PI3Kα, Ki: 0.29 nM
PI3Kβ, Ki: 9.1 nM
PI3Kγ, Ki: 0.97 nM
PI3Kδ, Ki: 0.12 nM
            Pan Inhibitor 99.46%
Bimiralisib
PI3Kα, IC50: 33 nM
PI3Kα-H1047R, IC50: 36 nM
PI3Kα-E545K, IC50: 136 nM
PI3Kα-E542K, IC50: 63 nM
PI3Kβ, IC50: 661 nM
PI3Kγ, IC50: 708 nM
PI3Kδ, IC50: 451 nM
     
Vps34, IC50: 6486 nM
    Pan Inhibitor 98.90%
AS-605240
PI3Kα, IC50: 60 nM
PI3Kβ, IC50: 270 nM
PI3Kγ, IC50: 8 nM
PI3Kδ, IC50: 300 nM
            Pan Inhibitor >98.0%
Gedatolisib
PI3Kα, IC50: 0.4 nM
PI3Kα-H1047R, IC50: 0.6 nM
PI3Kα-E545K, IC50: 0.6 nM
PI3Kβ, IC50: 6 nM
PI3Kγ, IC50: 5.4 nM
PI3Kδ, IC50: 6 nM
            Pan Inhibitor 99.11%
ZSTK474
PI3Kα, IC50: 16 nM
PI3Kβ, IC50: 44 nM
PI3Kγ, IC50: 49 nM
PI3Kδ, IC50: 4.6 nM
            Pan Inhibitor 99.71%
Apitolisib
PI3Kα, IC50: 5 nM
PI3Kβ, IC50: 27 nM
PI3Kγ, IC50: 14 nM
PI3Kδ, IC50: 7 nM
            Pan Inhibitor 99.13%
Vps34-PIK-III
PI(3)Kα, IC50: 3.96 μM
 
PI(3)Kγ, IC50: 3.04 μM
PI(3)Kδ, IC50: 1.2 μM
     
Vps34, IC50: 18 nM
    Pan Inhibitor 99.73%
AZD 6482
PI3Kα, IC50: 136 nM
PI3Kβ, IC50: 0.69 nM
PI3Kγ, IC50: 47.8 nM
PI3Kδ, IC50: 13.6 nM
 
PI3K-C2β, IC50: 54.1 nM
 
hVps34, IC50: 3390 nM
    Pan Inhibitor 99.26%
PI-103 Hydrochloride
p110α, IC50: 2 nM
p110β, IC50: 3 nM
p110γ, IC50: 15 nM
p110δ, IC50: 3 nM
            Pan Inhibitor 99.78%
AZD8186
PI3Kα, IC50: 35 nM
PI3Kβ, IC50: 4 nM
PI3Kγ, IC50: 675 nM
PI3Kδ, IC50: 12 nM
            Pan Inhibitor 99.97%
Voxtalisib
p110α, IC50: 39 nM
p110β, IC50: 113 nM
p110γ, IC50: 9 nM
p110δ, IC50: 43 nM
            Pan Inhibitor 98.93%
PIK-93
p110α, IC50: 39 nM
p110β, IC50: 590 nM
p110γ, IC50: 16 nM
p110δ, IC50: 120 nM
PI3KC2α, IC50: 16 μM
PI3KC2β, IC50: 140 nM
 
hsVPS34, IC50: 320 nM
    Pan Inhibitor 99.13%
Pictilisib dimethanesulfonate
p110α, IC50: 3 nM
p110α-H1047R, IC50: 3 nM
p110α-E545K, IC50: 3 nM
p110β, IC50: 33 nM
p110γ, IC50: 75 nM
p110δ, IC50: 3 nM
            Pan Inhibitor 99.12%
GDC-0084
PI3Kα, Ki: 2 nM
PI3Kβ, Ki: 46 nM
PI3Kγ, Ki: 10 nM
PI3Kδ, Ki: 3 nM
            Pan Inhibitor 99.28%
Leniolisib
PI3Kα, IC50: 280 nM
PI3Kβ, IC50: 480 nM
PI3Kγ, IC50: 2.57 μM
PI3Kδ, IC50: 11 nM
            Pan Inhibitor 99.62%
SF2523
PI3Kα, IC50: 34 nM
 
PI3Kγ, IC50: 158 nM
              Pan Inhibitor 99.37%
Dactolisib Tosylate
p110α, IC50: 4 nM
p110α-H1047R, IC50: 4.6 nM
p110α-E545K, IC50: 5.7 nM
p110β, IC50: 75 nM
p110γ, IC50: 5 nM
p110δ, IC50: 7 nM
            Pan Inhibitor 99.89%
Pilaralisib
PI3Kα, IC50: 39 nM
PI3Kβ, IC50: 383 nM
PI3Kγ, IC50: 23 nM
PI3Kδ, IC50: 36 nM
     
Vps34, IC50: 6974 nM
    Pan Inhibitor 99.57%
Buparlisib Hydrochloride
p110α, IC50: 52 nM
p110α-H1047R, IC50: 58 nM
p110α-E545K, IC50: 99 nM
p110β, IC50: 166 nM
p110γ, IC50: 262 nM
p110δ, IC50: 116 nM
     
Vps34, IC50: 2.4 μM
    Pan Inhibitor 98.01%
PI4KIIIbeta-IN-9
PI3Kα, IC50: 2 μM
 
PI3Kγ, IC50: 1046 nM
PI3Kδ, IC50: 152 nM
   
PI3KC2γ, IC50: 1 μM
      Pan Inhibitor 98.16%
Acalisib
p110α, IC50: 5441 nM
p110β, IC50: 3377 nM
p110γ, IC50: 1389 nM
p110δ, IC50: 12.7 nM
     
hVps34, IC50: 12682 nM
    Pan Inhibitor 99.98%
SAR-260301
PI3Kα, IC50: 1539 nM
PI3Kβ, IC50: 23 nM
PI3Kγ, IC50: 10000 nM
PI3Kδ, IC50: 468 nM
   
PI3KC2γ, IC50: 3812 nM
Vps34, IC50: 183 nM
    Pan Inhibitor 99.74%
BGT226 maleate
PI3Kα, IC50: 4 nM
PI3Kβ, IC50: 63 nM
PI3Kγ, IC50: 38 nM
              Pan Inhibitor 99.76%
AS-252424
PI3Kα, IC50: 935 nM
PI3Kβ, IC50: 20 μM
PI3Kγ, IC50: 30 nM
PI3Kδ, IC50: 20 μM
            Pan Inhibitor 97.52%
AZD-8835
PI3Kα, IC50: 6.2 nM
PI3Kα-E545K, IC50: 6 nM
PI3Kα-H1047R, IC50: 5.8 nM
PI3Kβ, IC50: 431 nM
PI3Kγ, IC50: 90 nM
PI3Kδ, IC50: 5.7 nM
            Pan Inhibitor 98.93%
Nemiralisib
PI3Kα, pIC50: 5.3
PI3Kβ, pIC50: 5.8
PI3Kγ, pIC50: 5.2
PI3Kδ, pKi: 9.9
            Pan Inhibitor 99.50%
PIK-90
p110α, IC50: 11 nM
p110β, IC50: 350 nM
p110γ, IC50: 18 nM
p110δ, IC50: 58 nM
PI3KC2α, IC50: 47 nM
PI3KC2β, IC50: 64 nM
 
hsVPS34, IC50: 830 nM
    Pan Inhibitor 99.06%
PF-04979064
PI3Kα, Ki: 0.13 nM
 
PI3Kγ, Ki: 0.111 nM
PI3Kδ, Ki: 0.122 nM
            Pan Inhibitor 99.75%
PKI-402
PI3Kα, IC50: 2 nM
PI3Kα-H1047R, IC50: 3 nM
PI3Kα-E545K, IC50: 3 nM
PI3Kβ, IC50: 7 nM
PI3Kγ, IC50: 16 nM
PI3Kδ, IC50: 14 nM
            Pan Inhibitor 99.44%
CH5132799
PI3Kα, IC50: 14 nM
PI3Kα-H1047R, IC50: 5.6 nM
PI3Kα-E545K, IC50: 6.7 nM
PI3Kα-E542K, IC50: 6.7 nM
PI3Kβ, IC50: 120 nM
PI3Kγ, IC50: 36 nM
PI3Kδ, IC50: 500 nM
 
PI3KC2β, IC50: 5.3 μM
        Pan Inhibitor >98.0%
GSK1059615
PI3Kα, IC50: 0.4 nM
PI3Kβ, IC50: 0.6 nM
PI3Kγ, IC50: 2 nM
PI3Kδ, IC50: 5 nM
            Pan Inhibitor 98.91%
GNE-477
PI3Kα, IC50: 4 nM
                  Pan Inhibitor 95.81%
CNX-1351
PI3Kα, IC50: 6.8 nM
PI3Kβ, IC50: 166 nM
PI3Kγ, IC50: 3020 nM
PI3Kδ, IC50: 240.3 nM
            Pan Inhibitor 99.88%
GNE-493
PI3Kα, IC50: 3.4 nM
PI3Kβ, IC50: 12 nM
PI3Kγ, IC50: 16 nM
PI3Kδ, IC50: 16 nM
            Pan Inhibitor 95.12%
VS-5584
PI3Kα, IC50: 16 nM
PI3Kβ, IC50: 68 nM
PI3Kγ, IC50: 25 nM
PI3Kδ, IC50: 42 nM
     
Vps34, IC50: 7470 nM
    Pan Inhibitor 98.01%
PI-3065
p110α, IC50: 910 nM
p110β, IC50: 600 nM
 
p110δ, IC50: 5 nM
            Pan Inhibitor 98.27%
PIK-294
p110α, IC50: 10 μM
p110β, IC50: 490 nM
p110γ, IC50: 160 nM
p110δ, IC50: 10 nM
            Pan Inhibitor 99.88%
AMG319
PI3Kα, IC50: 33 μM
PI3Kβ, IC50: 2.7 μM
PI3Kγ, IC50: 850 nM
PI3Kδ, IC50: 18 nM
            Pan Inhibitor 98.40%
NSC781406
PI3Kα, IC50: 2 nM
PI3Kβ, IC50: 9.4 nM
PI3Kγ, IC50: 2.7 nM
PI3Kδ, IC50: 14 nM
            Pan Inhibitor 99.55%
IPI-3063
p110α, IC50: 1170 nM
p110β, IC50: 1508 nM
p110γ, IC50: 2187 nM
p110δ, IC50: 2.5 nM
            Pan Inhibitor 98.80%
ETP-46321
p110α, Ki: 2.3 nM
PI3Kα-H1047R, Ki: 2.33 nM
PI3Kα-E545K, Ki: 1.77 nM
PI3Kα-E542K, Ki: 1.89 nM
p110β, Ki: 170 nM
p110γ, Ki: 179 nM
p110δ, Ki: 14.2 nM
            Pan Inhibitor >98.0%
CAL-130 Hydrochloride
p110α, IC50: 115 nM
p110β, IC50: 56 nM
p110γ, IC50: 6.1 nM
p110δ, IC50: 1.3 nM
            Pan Inhibitor 99.88%
PI3K-IN-6
PI3Kα, IC50: 850 nM
PI3Kβ, IC50: 7.8 nM
 
PI3Kδ, IC50: 5.3 nM
            Pan Inhibitor
PI3Kγ inhibitor 3
PI3Kα, pIC50: 5.1
PI3Kβ, pIC50: 4.5
PI3Kγ, pIC50: 9.1
PI3Kδ, pIC50: 6.5
PI3KC2α, pIC50: 5
PI3KC2β, pIC50: 7.5
PI3KC2γ, pIC50: 5.5
 
PI3KC3, pIC50: 5.1
  Pan Inhibitor
CHMFL-PI3KD-317
PI3Kα, IC50: 62.6 nM
PI3Kβ, IC50: 284 nM
PI3Kγ, IC50: 202.7 nM
PI3Kδ, IC50: 6 nM
 
PIK3C2B, IC50: 882.3 nM
 
Vps34, IC50: 1801.7 nM
    Pan Inhibitor
PI3K/HDAC-IN-1
PI3Kα, IC50: 42 nM
PI3Kβ, IC50: 101 nM
PI3Kγ, IC50: 67 nM
PI3Kδ, IC50: 8.1 nM
            Pan Inhibitor
PI3K/mTOR Inhibitor-2
PI3Kα, IC50: 3.4 nM
PI3Kβ, IC50: 34 nM
PI3Kγ, IC50: 1 nM
PI3Kδ, IC50: 16 nM
            Pan Inhibitor
PI3K/mTOR Inhibitor-1
PI3Kα, IC50: 20 nM
PI3Kβ, IC50: 376 nM
PI3Kγ, IC50: 204 nM
PI3Kδ, IC50: 46 nM
            Pan Inhibitor
Sonolisib
p110α, IC50: 0.1 nM
   
p110δ, IC50: 2.9 nM
         
p120γ, IC50: 1 nM
Pan Inhibitor
NVP-BAG956
PI3Kα, IC50: 56 nM
PI3Kβ, IC50: 446 nM
PI3Kγ, IC50: 117 nM
PI3Kδ, IC50: 35 nM
            Pan Inhibitor
PI3Kγ inhibitor 1
PI3Kα, IC50: 10 μM
PI3Kβ, IC50: 10 μM
PI3Kγ, IC50: 100 nM
PI3Kδ, IC50: 100 nM
            Pan Inhibitor
ON 146040
PI3Kα, IC50: 14 nM
PI3Kβ, IC50: 3 μM
PI3Kγ, IC50: 1 μM
PI3Kδ, IC50: 20 nM
            Pan Inhibitor
CAL-130
p110α, IC50: 115 nM
p110β, IC50: 56 nM
p110γ, IC50: 6.1 nM
p110δ, IC50: 1.3 nM
            Pan Inhibitor