AKT inhibitor 2

Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

PI3K/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

ZINC00640089 is a selective lipid carrier protein-2 (LCN2) inhibitor. ZINC00640089 inhibited cell proliferation and cell viability, and reduced AKT phosphorylation in SUM149 cells. ZINC00640089 can be used to study inflammatory breast cancer (IBC).

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2/Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

ZINC00784494 is a selective inhibitor of LCN2 (lipocalin-2), which inhibits cancer cell proliferation and reduces AKT phosphorylation levels, prevents the transition of the cell cycle from the G0 G1 phase to the S phase, and promotes apoptosis. It can be used for the study of inflammatory breast cancer (IBC).

BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) is a dual AKT and NFkB pathway inhibitor. It enhances the susceptibility of colon cancer cells to mda-7 IL-24-induced growth inhibition by targeting Akt.

CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1).

NSC117079 is a novel PHLPP1/2 (Pleckstrin homology domain and leucine rich repeat protein phosphatase) inhibitor that activates neuronal AKT and ameliorates staurosporine-induced cell death in neurons.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks (Kis of 4 nM, 6 nM, 2 nM, and 1 nM for PI3Kα, β, δ, and γ, respectively), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2]. AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM.

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

AKT-IN-25 (Compound 14a) is an inhibitor of Akt that prevents the phosphorylation of Akt, thereby hindering the PI3K Akt mTOR signaling pathway. It arrests the cell cycle at the G1 phase, inhibits the migration of PANC-1 cells, and suppresses the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2, with IC50 values of 3.05, 1.32, and 3.85 μM, respectively.

VEGFR-2 AKT-IN-2 (Compound 5) is an inhibitor of VEGFR-2 AKT, with an IC50 of 0.061 μM for VEGFR in human liver cancer cells. It reduces total and phosphorylated AKT in cells, increases BAX and caspase-3 levels, and decreases Bcl-2, thereby inducing apoptosis. Additionally, VEGFR-2 AKT-IN-2 halts the cell cycle at the S phase and inhibits the growth of human liver cancer cells.

ML-B01 is an orally active inhibitor targeting Akt and PKA, with IC50 values of 2 nM and 136 nM, respectively. It demonstrates good blood-brain barrier (BBB) permeability in mice.

Topo I II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K Akt mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.