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Home >> Signaling Pathways >> PI3K/Akt/mTOR Signaling >> PI3K

PI3K

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.

  1. Cat.No. Product Name Information
  2. GC62450 (S)-PI3Kα-IN-4 (S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer. (S)-PI3Kα-IN-4 Chemical Structure
  3. GC35037 1,3-Dicaffeoylquinic acid 1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative, and activates PI3K/Akt. 1,3-Dicaffeoylquinic acid Chemical Structure
  4. GC41992 1-Deoxynojirimycin (hydrochloride) 1-Deoxynojirimycin (1-dNM) (hydrochloride), produced by Bacillus species, is a glucose analog that potently inhibits α-glucosidase I and II. 1-Deoxynojirimycin (hydrochloride) Chemical Structure
  5. GC10710 3-Methyladenine

    3-Methyladenine is a classic autophagy inhibitor.

     3-Methyladenine Chemical Structure
  6. GC16157 740 Y-P PI 3-kinase activator,cell permeable 740 Y-P Chemical Structure
  7. GC17550 A66 P110α inhibitor A66 Chemical Structure
  8. GC10860 Acalisib (GS-9820) Acalisib (GS-9820) is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM. Acalisib (GS-9820) Chemical Structure
  9. GC13913 AMG319 PI3Kδ inhibitor AMG319 Chemical Structure
  10. GC35395 Arnicolide D Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner. Arnicolide D Chemical Structure
  11. GC11910 AS-041164 PI3Kγ inhibitor AS-041164 Chemical Structure
  12. GC13901 AS-252424 PI3Kγ inhibitor,novel and potent AS-252424 Chemical Structure
  13. GC38061 AS-604850 A selective inhibitor of PI3Kγ AS-604850 Chemical Structure
  14. GC12080 AS-604850 PI3Kγ inhibitor,selective and ATP-competitve AS-604850 Chemical Structure
  15. GC12474 AS-605240 Potent and selective PI 3-Kγ inhibitor AS-605240 Chemical Structure
  16. GC62335 AZ2 AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). AZ2 Chemical Structure
  17. GC64938 AZD-7648 AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity. AZD-7648 Chemical Structure
  18. GC65149 AZD3458 AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively. AZD3458 Chemical Structure
  19. GC16851 AZD6482

    PI3Kβ inhibitor,potent and selective

     AZD6482 Chemical Structure
  20. GC65507 AZD8154 AZD8154 is a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory disease. AZD8154 Chemical Structure
  21. GC12576 AZD8186 Potent and selective inhibitor of PI3Kβ and PI3Kδ AZD8186 Chemical Structure
  22. GC11248 AZD8835 PI3Kα and PI3Kδ inhibitor AZD8835 Chemical Structure
  23. GC17766 BAY 80-6946 (Copanlisib) BAY 80-6946 (Copanlisib) (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. BAY 80-6946 (Copanlisib) has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. BAY 80-6946 (Copanlisib) has superior antitumor activity. BAY 80-6946 (Copanlisib) Chemical Structure
  24. GC62164 BAY1082439 BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth. BAY1082439 Chemical Structure
  25. GC33145 BEBT-908 (PI3Kα inhibitor 1) BEBT-908 (PI3Kα inhibitor 1) (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) . BEBT-908 (PI3Kα inhibitor 1) Chemical Structure
  26. GC10060 BEZ235 (NVP-BEZ235) BEZ235 (NVP-BEZ235) (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. BEZ235 (NVP-BEZ235) (BEZ235) inhibits both mTORC1 and mTORC2. BEZ235 (NVP-BEZ235) Chemical Structure
  27. GC13271 BEZ235 Tosylate BEZ235 Tosylate Chemical Structure
  28. GC35509 BGT226 BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells. BGT226 Chemical Structure
  29. GC11931 BKM120 An inhibitor of class I PI3K isoforms BKM120 Chemical Structure
  30. GC65534 Boc-L-cyclobutylglycine Boc-L-cyclobutylglycine is a glycine derivative that can be used for PI3K inhibitor synthesis. Boc-L-cyclobutylglycine Chemical Structure
  31. GC30156 Brevianamide F (Cyclo(L-Pro-L-Trp)) Brevianamide F (Cyclo(L-Pro-L-Trp)) (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F (Cyclo(L-Pro-L-Trp)) Chemical Structure
  32. GC16462 BYL-719 BYL-719 (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. BYL-719 (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. BYL-719 (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity. BYL-719 Chemical Structure
  33. GC13396 CAL-101 (Idelalisib, GS-1101) A selective PI3K p110δ inhibitor CAL-101 (Idelalisib, GS-1101) Chemical Structure
  34. GC35579 CAL-130 CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively. CAL-130 Chemical Structure
  35. GC11135 CAL-130 Hydrochloride CAL-130 Hydrochloride Chemical Structure
  36. GC35580 CAL-130 Racemate CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor. CAL-130 Racemate Chemical Structure
  37. GC14318 CAY10505 Potent PI3Kγ inhibitor CAY10505 Chemical Structure
  38. GC10070 CGS 15943 adenosine receptor antagonist CGS 15943 Chemical Structure
  39. GC11868 CH5132799 Class I PI3K inhibitor CH5132799 Chemical Structure
  40. GC65969 CHMFL-PI3KD-317 CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells. CHMFL-PI3KD-317 Chemical Structure
  41. GC19109 CNX-1351 CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM. CNX-1351 Chemical Structure
  42. GC12115 CUDC-907 A dual inhibitor of HDACs and PI3Ks CUDC-907 Chemical Structure
  43. GC68413 CYH33 CYH33 Chemical Structure
  44. GC63391 CYH33 methanesulfonate CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors. CYH33 methanesulfonate Chemical Structure
  45. GC14798 CZC24832 A PI3Kγ inhibitor CZC24832 Chemical Structure
  46. GC38482 Desmethylglycitein Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes. Desmethylglycitein Chemical Structure
  47. GC60782 Disitertide TFA Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer. Disitertide TFA Chemical Structure
  48. GC62495 DS-7423 DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity. DS-7423 Chemical Structure
  49. GC33162 Duvelisib R enantiomer (IPI-145 R enantiomer) Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib. Duvelisib R enantiomer (IPI-145 R enantiomer) Chemical Structure
  50. GC38694 Erucic acid A 22carbon monounsaturated fatty acid Erucic acid Chemical Structure
  51. GC38236 Esculetin A coumarin with diverse actions Esculetin Chemical Structure
  52. GC19145 ETP-46321 ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively. ETP-46321 Chemical Structure
  53. GC38392 Euscaphic acid Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis. Euscaphic acid Chemical Structure
  54. GC62973 FD223 FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML. FD223 Chemical Structure
  55. GC17967 GDC-0032 GDC-0032 (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively. GDC-0032 Chemical Structure
  56. GC32710 GDC-0077 (RG6114) GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα. GDC-0077 (RG6114) Chemical Structure
  57. GC10228 GDC-0084 PI3K and mTOR inhibitor, brain-permeable GDC-0084 Chemical Structure
  58. GC19161 GDC-0326 GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM. GDC-0326 Chemical Structure
  59. GC10816 GDC-0941 GDC-0941 (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). GDC-0941 Chemical Structure
  60. GC16154 GDC-0941 dimethanesulfonate A pan inhibitor of class I PI3K isoforms GDC-0941 dimethanesulfonate Chemical Structure
  61. GC11177 GDC-0980 (RG7422) GDC-0980 (RG7422) (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with aKiof 17 nM for mTOR. GDC-0980 (RG7422) Chemical Structure
  62. GC64778 Gilmelisib Gilmelisib is an antineoplastic. Gilmelisib is a PI3K inhibitor (IC50 <1 nM for PI3K p110α) extracted from WO2017101847 A1, compound 1. Gilmelisib Chemical Structure
  63. GN10584 Ginsenoside Rk1 Ginsenoside Rk1 Chemical Structure
  64. GC38606 Glaucocalyxin A Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect. Glaucocalyxin A Chemical Structure
  65. GC17338 GNE-317 potent, brain-penetrant PI3K inhibitor GNE-317 Chemical Structure
  66. GC10340 GNE-477 dual PI3K/mTOR inhibitor GNE-477 Chemical Structure
  67. GC68429 GNE-490 GNE-490 Chemical Structure
  68. GC15423 GNE-493 Pan-PI3K/mTOR inhibitor GNE-493 Chemical Structure
  69. GC36186 GS-9901 GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. GS-9901 Chemical Structure
  70. GC65309 GSK-F1 GSK-F1 (Compound F1) is an orally active PI4KA inhibitor with pIC50 values of 8.0, 5.9, 5.8, 5.9, 5.9 and 6.4 against PI4KA, PI4KB, PI3KA, PI3KB, PI3KG and PI3KD, respectively. GSK-F1 Chemical Structure
  71. GC11018 GSK1059615 PI3K and mTOR inhibitor,potent and reversible GSK1059615 Chemical Structure
  72. GC15072 GSK2126458 GSK2126458 (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. GSK2126458 has anti-cancer activity. GSK2126458 Chemical Structure
  73. GC15595 GSK2269557 inhibitor of PI3Kδ GSK2269557 Chemical Structure
  74. GC15679 GSK2292767 PI3Kδ inhibitor,potent and selective GSK2292767 Chemical Structure
  75. GC64612 GSK251 GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode. GSK251 Chemical Structure
  76. GC17109 GSK2636771

    GSK2636771 is a potent adenosine triphosphate competitive oral inhibitor of PI3Kβ, with an IC50 of 5.

     GSK2636771 Chemical Structure
  77. GC38088 Hederacolchiside A1 Hederacolchiside A1 Chemical Structure
  78. GC38168 Heterophyllin B Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer. Heterophyllin B Chemical Structure
  79. GC64035 Hirsutenone Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone Chemical Structure
  80. GC16713 HS-173 novel PI3K inhibitor HS-173 Chemical Structure
  81. GC62572 hSMG-1 inhibitor 11e hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of 900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM). hSMG-1 inhibitor 11e Chemical Structure
  82. GC61925 hSMG-1 inhibitor 11j hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer. hSMG-1 inhibitor 11j Chemical Structure
  83. GC15540 IC-87114 PI3Kδ inhibitor IC-87114 Chemical Structure
  84. GC62465 Idelalisib D5 Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor. Idelalisib D5 Chemical Structure
  85. GC63017 IHMT-PI3Kδ-372 IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 Chemical Structure
  86. GC19411 IITZ-01 IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ. IITZ-01 Chemical Structure
  87. GC13503 iMDK PI3K and endogenous midkine (MDK) expression inhibitor iMDK Chemical Structure
  88. GC62376 iMDK quarterhydrate iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice. iMDK quarterhydrate Chemical Structure
  89. GC12416 INK1117 INK1117 (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM. INK1117 Chemical Structure
  90. GC10749 IPI-145 (INK1197) IPI-145 (INK1197) (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively. IPI-145 (INK1197) Chemical Structure
  91. GC31756 IPI-3063 IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5?±?1.2 nM. IPI-3063 Chemical Structure
  92. GC19202 IPI549 IPI549 (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. IPI549 shows >100-fold selectivity over other lipid and protein kinases. IPI549 Chemical Structure
  93. GN10023 Isorhamnetin Isorhamnetin Chemical Structure
  94. GC14346 KU-0060648 Dual DNA-PK/PI3-K inhibitor, ATP-competitive KU-0060648 Chemical Structure
  95. GC36426 LAS191954 LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM. LAS191954 Chemical Structure
  96. GC19471 Leniolisib

    A potent and selective PI3Kδ inhibitor

     Leniolisib Chemical Structure
  97. GC30884 LX2343 An inhibitor of BACE1 and PI3K LX2343 Chemical Structure
  98. GC15485 LY 294002

    LY294002 is the first synthetic PI3Kα, δ and β inhibitor

     LY 294002 Chemical Structure
  99. GC14371 LY3023414 LY3023414 (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations. LY3023414 Chemical Structure
  100. GC19256 MTX-211 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases. MTX-211 Chemical Structure
  101. GC65442 Musk ketone Musk ketone (MK) is a widely used artificial fragrance. Musk ketone Chemical Structure

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