Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
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
S2743 PF-04691502 <1 mg/mL 14 mg/mL <1 mg/mL
S1558 AT7867 <1 mg/mL 68 mg/mL 5 mg/mL
S1117 Triciribine <1 mg/mL 64 mg/mL <1 mg/mL
S2635 CCT128930 <1 mg/mL 68 mg/mL 6 mg/mL
S2670 A-674563 72 mg/mL 72 mg/mL 18 mg/mL
S1556 PHT-427 <1 mg/mL 82 mg/mL 60 mg/mL
S3056 Miltefosine 81 mg/mL <1 mg/mL 81 mg/mL
S2310 Honokiol <1 mg/mL 53 mg/mL <1 mg/mL
S7127 TIC10 Analogue <1 mg/mL 11 mg/mL <1 mg/mL
S7492 Uprosertib (GSK2141795) <1 mg/mL 85 mg/mL 85 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
S8339 Miransertib (ARQ 092) HCl <1 mg/mL 75 mg/mL 4 mg/mL
S7521 Afuresertib (GSK2110183) <1 mg/mL 85 mg/mL 85 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL
S8132 Deguelin <1 mg/mL 78 mg/mL 78 mg/mL
S7863 SC79 <1 mg/mL 72 mg/mL 72 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

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.


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.



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.


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.



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.



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.



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.



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.



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.



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.



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.



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.



Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.


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.


Uprosertib (GSK2141795)

Uprosertib (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.



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.



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.


Miransertib (ARQ 092) HCl

ARQ 092 is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.


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.



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.



Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.



SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

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