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Akt Inhibitors (15)


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, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.
  • Cell, 2015, 160(1-2):161-76
  • Nat Genet, 2014, 46(4):364-70
  • Cancer Cell, 2015, 27(1):97-108
S1037 Perifosine (KRX-0401) Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM, 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, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
  • Cancer Discov, 2014, 4(2):186-99
  • Oncogene, 2014, 33(22):2846-56
  • Elife, 2014, 10.7554/eLife.03751
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, 620-fold selectivity over PKA. Phase 2.
  • Cell, 2015, 160(1-2):161-76
S8019 AZD5363 AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.
  • OncoImmunology, 2015, 10.1080/2162402X.2015.1005448
  • Cell Commun Signal, 2014, 12(1):61
  • PLoS One, 2014, 9(10):e108780
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.
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, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
  • Mol Cancer Res, 2014, 12(10):1520-31
  • Cell Signal, 2014, 26(8):1627-35
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, respectively; little activity outside the AGC kinase family.
  • Cancer Research, 2012, 72(5):1229-38
  • Cell Signal, 2014, 26(8):1627-35
  • J Pharmacol Exp Ther, 2014, 350(3):624-34
S7127 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.
S1117 Triciribine Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 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
  • Eur J Pharmacol, 2015, 747C:71-87
S2670 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
  • 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, 2014, 58(7):3689-96
  • Antimicrob Agents Chemother, 2015, 59(2):1088-99

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