akt3

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1

PI3K/Akt/mTOR-IN-3 is a potent inhibitor of PI3K/Akt/mTOR. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 cells (IC50: 0.77 μM), HeLa cells (IC50: 1.23 μM) and HepG2 cells (IC50: 4.57 μM). PI3K/Akt/mTOR-IN-3 inhibited the migration of MCF-7 and HeLa cells at a concentration of 4 μM. PI3K/Akt/mTOR-IN-3 blocked the cell cycle in S phase and induced apoptosis.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8 12 65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Hu7691 free base is an orally active, potent, and selective Akt inhibitor with anti-proliferative and neurogenic effects on various neuroblastoma cell lines. It inhibits Akt1, Akt2, and Akt3, and induces differentiation of neuroblastoma cells.

Hu7691 is an orally active, selective, and potent Akt inhibitor that targets Akt1, Akt2, and Akt3, while also inhibiting neuroblastoma cell proliferation and inducing their differentiation.

MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.This compound is unstable in powder form and other related salt forms are recommended.

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

MK-2206 is an orally active, highly selective, metabotropic Akt inhibitor that targets Akt1 [IC50: 8 nM], Akt2 [IC50: 12 nM], and Akt3 [IC50: 65 nM]. Many breast cancer cell lines, PIK3CA mutants, and PTEN-losing cell lines are sensitive to MK-2206, which exhibits anti-cancer effects.

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

Ipatasertib (GDC-0068) (GDC-0068), a highly specific pan-Akt inhibitor, targets Akt1 2 3 with IC50 of 5 nM 18 nM 8 nM, respectively.

GSK-690693 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.

Uprosertib (GSK2141795) (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.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3 7 7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

AKT inhibitor VIII (AKTi-1 2) is a highly specific inhibitor of Akt1 2, with IC50 values of 58 nM and 210 nM respectively, demonstrating approximately 36-fold greater selectivity for Akt1 over Akt3.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

AT7867 is a potent ATP-competitive inhibitor of Akt1 2 3 and p70S6K PKA with IC50 values of 32 nM, 17 nM, 47 nM, 85 nM, and 20 nM, respectively, exhibiting little activity outside the AGC kinase family.

Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041

ALM301 is a highly specific, orally active AKT inhibitor that acts on AKT1 (IC50: 0.13 μM), AKT2 (IC50: 0.09 μM) and AKT3 (IC50: 2.75 μM). ALM301 inhibits AKT phosphorylation in vitro and has a regulatory effect on downstream signalling. ALM301 exhibits inhibitory effects on cancer cell proliferation and tumor growth.

AKT-IN-13 (compound 4b) is a potent inhibitor of Akt, acting on Akt1 (IC50: 1.6 nM), Akt2 (IC50: 2.4 nM), and Akt3 (IC50: 0.3 nM). It can be used in anticancer research.

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours.

MK-2206 free base is a potent, selective, and orally administered allosteric Akt inhibitor with IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. It demonstrates sensitivity in various breast cancer cell lines, including those with PIK3CA mutations and PTEN loss, indicating its potential for anticancer activities [1] [2].

MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.

AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1 Akt2 Akt3 and p70S6K PKA kinase, with IC50 values of 32 nM 17 nM 47 nM and 85 nM 20 nM, respectively. It induces pharmacodynamic changes and inhibits human tumor xenograft growth.

AKT-IN-8 is a potent inhibitor of AKT, demonstrating inhibitory concentrations (IC50) of 4.46 nM for AKT1, 2.44 nM for AKT2, and 9.47 nM for AKT3.

INY-03-041, a potent and highly selective PROTAC-based pan-AKT degrader, inhibits AKT1, AKT2, and AKT3 with IC50s of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. This compound consists of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide.

MS15 TFA is a potent, selective AKT PROTAC degrader, effectively inhibiting AKT1, AKT2, and AKT3 with IC50 values of 798 nM, 90 nM, and 544 nM, respectively [1].

TAS-117 hydrochloride is a selective, potent, orally active allosteric Akt inhibitor, acting on Akt1 (IC50: 4.8 nM), Akt2 (IC50: 1.6 nM) and Akt3 (IC50: 44 nM). TAS-117 hydrochloride stimulates anti-myeloma activity, enhances lethal endoplasmic reticulum stress induced by proteasome inhibition, and can induce apoptosis and autophagy.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08 2 2.6 nM for Akt1 Akt2 Akt3 respectively)

BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay)

GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties.

M2698 (MSC2363318A) is an inhibitor of p70S6K, Akt1 and Akt3 with IC50s of 1 nM. M2698 shows anti-cancer activity.

Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].

Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively).

INY-03-041 trihydrochloride, a potent and highly selective PROTAC-based pan-AKT degrader, comprises Ipatasertib, an ATP-competitive AKT inhibitor, conjugated to Lenalidomide. It effectively inhibits AKT1, AKT2, and AKT3 with IC50 values of 2.0, 6.8, and 3.5 nM, respectively [1].

MS15 is a potent, selective degrader of AKT PROTAC, effectively inhibiting activities of AKT1, AKT2, and AKT3. It exhibits IC50 values of 798 nM for AKT1, 90 nM for AKT2, and 544 nM for AKT3, respectively [1].

TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors.

(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.

9-Decyn-1-ol is an alkyl ether-based PROTAC linker used in synthesizing PROTACs, acting as a conjugation agent to combine GDC-0068 and Lenalidomide to form INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].

NTQ1062 (compound 22b) is an orally active and potent Akt inhibitor that acts on Akt1 (IC50: 0.4 nM), Akt2 (IC50: 6.3 nM) and Akt3 (IC50: 0.1 nM). NTQ1062 showed significant anti-tumor effects in the LNCap xenograft tumor mouse model.