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.
Cat. No. | Product Name | CAS No. | Information |
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H9244 |
AKTide-2T TFA |
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM; AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position. |
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H9243 |
AKTide-2T |
324029-01-8 | AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM; AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position. |
H6915 |
SC-79 |
305834-79-1 | A unique specific Akt activator; binds to the PH domain of Akt and inhibits Akt membrane translocation, but paradoxically activates Akt in the cytosol; induces the p-Akt (Ser473) expression and significantly increases the expression of Bcl-2 and p-GSK-3β (Ser9), decreases the protein levels of Bax, cytoplasm cytochrome C, and cleaved caspase-3.; augments neuronal survival in mouse model for ischemic strok. |
H6914 |
SC-66 |
871361-88-5 | 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. |
H6913 |
PHT-427 |
1191951-57-1 | PHT-427 is a small-molecule Akt inhibitor that binds selectively to the PH domain of AKT with Ki of 2.4 uM, inhibits phospho-Ser473-AKT in Panc-1 cells with IC50 of 6.3 uM; decreases AKT activation and causes apoptosis at low micromolar concentrations in Panc-1 and MiaPaCa-2 pancreatic cancer cell lines; inhibits AKT and its downstream targets in cells, exhibits good antitumor activity in pancreatic cancer cell xenografts in immunocompromised mice. |
H6912 |
Perifosine |
157716-52-4 | A oral bioavailable alkylphospholipid that displays significant antiproliferative activity in vitro and in vivo in several human tumor model; acts as an Akt inhibitor and a PI3K inhibitor, induces p21(WAF1) expression in squamous carcinoma cells through a p53-independent pathway; enhances apoptosis and inhibits the growth of xenografts in nude mice combined with a lysosomal inhibitor. |
H6911 |
MK 2206 dihydrochloride |
1032350-13-2 | A potent, orally active allosteric Akt inhibitor with IC50 of 5/12 nM for Akt1/Akt2 respectively; shows 5-fold less potent against human Akt3 (IC50=65 nM); synergistically inhibits cell proliferation of human cancer cell lines in combination with erlotinib or lapatinib in vitro; suppresses the Akt phosphorylation that is induced by carboplatin and gemcitabine. |
H6910 |
Miransertib |
1313881-70-7 | 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. |
H6908 |
GSK-690693 |
937174-76-0 | A potent, ATP competitive, pan-AKT inhibitor with IC50 of 2, 13, and 9 nM against AKT1, 2, and 3, respectively; also inhibits additional members of the AGC kinase family (PKA, PrkX, and PKC isozymes, IC50s<100 nM); dose-dependently reduces the phosphorylation GSK3 beta, PRAS40 and Forkhead, inhibits proliferation and induces apoptosis in a subset of tumor cells; exhibits significant antitumor activity in mice model. |
H6907 |
Ch-319 |
Ch-319 (Ch319) is a triphenyltin (IV) carboxylate derivative that modulates AKT/FOXO3a signaling and inhibits progression of prostate cancer; reduces viability and induces cell cycle arrest associated with downregulation of PI3K and dephosphorylation of AKT and PRAS40 in PTEN-null PC3M and DU145 PCa cells at 250-500 nM; decreases tumor weights, reduces expression of androgen receptor, decreases phosphorylation of AKT and PRAS40 and increases FOXO3a in mice. |
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