Akt/PKB (Protein kinase B), a serine/threonine protein kinase with antiapoptotic activity, is one of the major downstream targets of PtdIns(3,4,5)P3 signaling pathway. It contains a pleckstrin homology domain (PH domain) that specifically binds PtdIns(3,4,5)P3 on the plasma membrane. Akt phosphorylation and activation are directly determined by the level of PtdIns(3,4,5)P3 on the plasma membrane, which is regulated by PI3K.
Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Akt isoforms have an N-terminal PH (pleckstrin homology) domain and a kinase domain, which are separated by a 39-amino-acid hinge region. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis.
Akt is a crucial mediator of cell survival and its deactivation is implicated in various stress-induced pathological cell death and degenerative diseases.
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AT7867 is a potent, ATP-competitive, orally available dual Akt and p70S6K inhibitor with Ki of 17-85 nM, also inhibits PKA with Ki of 20 nM; potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3beta (IC50=7.1 uM, pSer9 GSK3β in U87MG glioblastoma cells) and S6 ribosomal protein phosphorylation, causes growth inhibition in a range of human cancer cell lines; inhibits AKT and p70S6K and induces apoptosis, inhibits human tumor growth in PTEN-deficient xenograft models.
A potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP; binds to active AKT1 with Kd of 2.7 nM and inactive AKT1 with Kd of 1.3 nM. displays >86-fold less potent against AKT3; inhibits the phosphorylation of AKT1 at T308 and S473 (IC50=0.9 and 1.1 nM, respectively), PRAS40 at T246 and 4EBP1 at T70; targets tumors displaying PI3K/AKT/mTOR pathway activation, inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors; exhibits strong in vivo patient-derived xenograft models.
Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor; specifically binds to two non-catalytic cysteines in AKT at 120 positions 296 and 310; exhibits pronounced sensitivity to breast cancer cell line ZR-75-1 with EC50 of 5 nM, 7- to 12-fold higher potency compared to reversible allosteric inhibitor miransertib and MK-2206; demonstrated strong antiproliferative activity in cancer cell lines harboring genetic alterations within the PTEN, PI3K, and RAS signaling pathways,b displayed antitumor activity in combination with the MEK inhibitor trametinib in patient-derived xenograft models of mutant KRAS pancreatic and colon cancer.
Miransertib (ARQ-092) is a potent, selective and allosteric inhibitor of Akt1/2/3 with IC50 of 5/4.5/16 nM respectively; inhibits cellular AKT activation and the phosphorylation of the downstream target PRAS40; inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma; orally bioavailable.
A potent, selective, ATP-competitive pan-AKT inhibitor with biochemical IC50 of 0.08/2/2.6 nM for AKT1/2/3; also inhibits PKA (IC50=1.3 nM) and AKT1 E17K mutant (IC50=0.2 nM), selective over PKC, PKG isoforms and p70S6K; orally bioactive.
A broadly selective, potent, ATP-competitive Akt kinase inhibitor with IC50 of 0.5 nM(biochemical assay), and 0.31 nM (cell function assay); shows >900-fold selectivity over PKA; excellent PK profiles and effective in in vivo models of xenograft tumor.
A-674563 is a potent, selective and orally available AKT inhibitor with Ki of 11 nM (Akt1); increases the efficacy of paclitaxel in a PC-3 xenograft model; enhances the transcription of several chondrocyte marker genes, including Col2a1, Acan and Col11a2, in mouse primary chondrocytes by inhibiting Sox9 degradation through the ubiquitin-proteasome pathway; also suppresses FLT3-ITD positive AML both in vitro and in vivo.
Akt1 and Akt2-IN-1
A potent, selective dual Akt1 and Akt2 inhibitor with IC50 of 3.5 nM and 42 nM, respectively; shows selectivity for Akt1/2 over Akt3 (IC50=1900 nM), and highly selective over other members of the AGC family of kinases; inhibit the growth of A2780 tumors in vivo; shows good physical properties and PK profile.
SC66 is an allosteric Akt inhibitor; exhibits a dual inhibitory activity that directly interferes with the PH domain binding to PIP3 and facilitates Akt ubiquitination; has anticancer activity mouse xenograft tumor model.
AKT Kinase Inhibitor
An Akt kinase inhibitor.
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