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Akt Inhibitors | Activators (19)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1078 MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.
  • Nature, 2015, 10.1038/nature15376
  • Cell, 2015, 160(1-2):161-76
  • Nat Genet, 2014, 46(4):364-70
S1037 Perifosine (KRX-0401) Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.
  • Cell, 2012, 149(3):656-70
  • Cancer Cell, 2013, 23(6):839-52
  • PLoS Biol, 2011, 9(9):e1001148
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
  • Cancer Discov, 2014, 4(2):186-99
  • Elife, 2014, 10.7554/eLife.03751
  • Oncogene, 2014, 33(22):2846-56
S2808 Ipatasertib (GDC-0068) Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.
  • Cell, 2015, 160(1-2):161-76
  • Mol Cancer Ther, 2015, 14(8):1928-38
  • J Biol Chem, 2014, 289(49):34189-204
S8019 AZD5363 AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.
  • Nat Commun, 2015, 6:6750
  • Oncogene, 2015, 10.1038/onc.2015.226
  • OncoImmunology, 2015, 10.1080/2162402X.2015.1005448
S7963 TIC10 TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
S7776 Akti-1/2 Akti-1/2 is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3.
S7863 SC79 SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.
S7521 Afuresertib (GSK2110183) Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.
S2743 PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
  • Blood, 2015, 10.1182/blood-2014-11-610329
  • Cell Rep, 2015, 11(3):446-59
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S1558 AT7867 AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family.
  • Cancer Res , 2012, 72(5):1229-38
  • Mol Carcinog, 2015, 10.1002/mc.22328
  • Cell Signal, 2014, 26(8):1627-35
S7563 AT13148 AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
S7127 TIC10 Analogue TIC10 Analogue is an analogue of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
S1117 Triciribine Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
S1556 PHT-427 PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.
  • Blood, 2011, 118(10):2840-8
  • Free Radic Res, 2015, 49(9):1095-113
  • Eur J Pharmacol, 2015, 747C:71-87
S2670 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.
  • Eur J Pharmacol, 2015, 764:208-214
  • Microvasc Res, 2015, 101:72-81
  • Hum Cell, 2015, 28(3):114-21
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
  • Eur J Pharmacol, 2015, 764:208-214
  • DNA Cell Biol, 2014, 33(12):847-53
S2310 Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.
  • Sensor actuat B-chem, 2012, Jin Akagi
S3056 Miltefosine Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
  • Antimicrob Agents Chemother, 2015, 59(2):1088-99
  • Antimicrob Agents Chemother, 2014, 58(7):3689-96
  • Biochem Biophys Res Commun, 2015, 10.1016/j.bbrc.2015.12.096

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1078 MK-2206 2HCl <1 mg/mL 14 mg/mL <1 mg/mL
S1037 Perifosine (KRX-0401) 8 mg/mL <1 mg/mL 15 mg/mL
S1113 GSK690693 <1 mg/mL 39 mg/mL <1 mg/mL
S2808 Ipatasertib (GDC-0068) <1 mg/mL 92 mg/mL 92 mg/mL
S8019 AZD5363 <1 mg/mL 86 mg/mL <1 mg/mL
S7963 TIC10 <1 mg/mL 77 mg/mL 77 mg/mL
S7776 Akti-1/2 <1 mg/mL 22 mg/mL <1 mg/mL
S7863 SC79 <1 mg/mL 72 mg/mL 72 mg/mL
S7521 Afuresertib (GSK2110183) <1 mg/mL 85 mg/mL 85 mg/mL
S2743 PF-04691502 <1 mg/mL 14 mg/mL <1 mg/mL
S1558 AT7867 <1 mg/mL 68 mg/mL 5 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL
S7127 TIC10 Analogue <1 mg/mL 11 mg/mL <1 mg/mL
S1117 Triciribine <1 mg/mL 64 mg/mL <1 mg/mL
S1556 PHT-427 <1 mg/mL 82 mg/mL 60 mg/mL
S2670 A-674563 72 mg/mL 72 mg/mL 18 mg/mL
S2635 CCT128930 <1 mg/mL 68 mg/mL 6 mg/mL
S2310 Honokiol <1 mg/mL 53 mg/mL <1 mg/mL
S3056 Miltefosine 82 mg/mL <1 mg/mL 82 mg/mL
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