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Akt Inhibitors (15)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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.
  • Nat Genet, 2014, 46(4):364-70
  • Cancer Cell, 2013, 24(6):766-76
  • Nat Cell Biol, 2013, 15(6):614-24
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 2.
  • 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, 2013, 10.1158/2159-8290.CD-13-0520
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
  • Mol Cancer Ther, 2012, 11(7):1510-7
S2808 GDC-0068 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.
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.
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
  • Cell Signal, 2014, 10.1016/j.cellsig.2014.03.013
  • Apoptosis, 2014, 10.1007/s10495-014-0991-2
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, 10.1016/j.cellsig.2014.03.013
  • PLoS One, 2013, 8(2):e57508
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.
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.
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.
Cat.No. Product Name Information Product Citations Customer Reviews
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
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. Phase 4.
  • Antimicrob Agents Chemother, 2014, 10.1128/AAC.02798-13
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
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.
S2732 Triciribine phosphate Triciribine phosphate, the active metabolite of TCN, is a potent Akt inhibitor with IC50 of 130 nM, that inhibits the phosphorylation of Akt in intact cells but not in vitro, more active in cells lacking adenosine kinase. Phase 1/2.
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