2. PI3K/Akt/mTOR Cytoskeleton Cell Cycle/DNA Damage Stem Cell/Wnt TGF-beta/Smad MAPK/ERK Pathway Apoptosis
  3. Akt PAK PKA MEK ERK Apoptosis Bcl-2 Family Caspase
  4. AKT1-IN-13

AKT1-IN-13 is an orally active AKT1 inhibitor with an IC50 of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma.

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AKT1-IN-13

AKT1-IN-13 Chemical Structure

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AKT1-IN-13 Related Antibodies

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Akt Akt1 Akt2 Akt3

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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PKA PKAR PKACα

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

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ERK ERK1 ERK2 ERK5 ERK8

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

AKT1-IN-13 is an orally active AKT1 inhibitor with an IC50 of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma[1].

IC50 & Target[1]

Akt1

5.17 μM (IC50)

PAK1

 

MEK1

 

ERK2

 

Bax

 

Bcl-2

 

Caspase 3

 

In Vitro

AKT1-IN-13 (Compound 17) (1.0 μM; 50 min) is a multi-target kinase inhibitor that potently inhibits AKT1 (with an inhibition rate of 95% at 1 μM), and exhibits an inhibition rate of > 80% against another 4 kinases (PAK1, PKA, MAP2K1, MAPK1) at 1 μM[1].
AKT1-IN-13 (72 h) potently inhibits the proliferation of human hepatocellular carcinoma HepG2 cells, with an IC50 of 2.09 μM and a selectivity index as high as 11.53[1].
AKT1-IN-13 (2-6 μM; 48 h) induces apoptosis in human hepatocellular carcinoma HepG2 cells in a concentration-dependent manner[1].
AKT1-IN-13 (2-6 μM; 48 h) inhibits the migration of human hepatocellular carcinoma HepG2 cells in a concentration-dependent manner[1].
AKT1-IN-13 (2-6 μM; 24 h) inhibits the invasion of human hepatocellular carcinoma HepG2 cells in a concentration-dependent manner[1].
AKT1-IN-13 (2-6 μM; 48 h) reduces the mitochondrial transmembrane potential of human hepatocellular carcinoma HepG2 cells in a concentration-dependent manner in vitro[1].
AKT1-IN-13 (2-6 μM; 48 h) induces G0/G1 cell cycle arrest in human hepatocellular carcinoma HepG2 cells in a concentration-dependent manner in vitro[1].
AKT1-IN-13 (2-6 μM; 48 h) inhibits AKT phosphorylation and activates the apoptotic pathway in a concentration-dependent manner in human hepatocellular carcinoma HepG2 cells in vitro, reduces p-AKT levels, and upregulates the expression of pro-apoptotic proteins[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AKT1-IN-13 Related Antibodies

Apoptosis Analysis[1]

Cell Line: human liver cancer HepG2 cells
Concentration: 2, 4 and 6 μM
Incubation Time: 48 h
Result: Induced a concentration-dependent increase in apoptosis rates: early apoptosis rates rose from 2.42% (control) to 19.49% at 6 μM.
Caused morphological changes including loss of cell membrane smoothness and smaller nuclei.

Cell Migration Assay [1]

Cell Line: human liver cancer HepG2 cells
Concentration: 2, 4 and 6 μM
Incubation Time: 48 h
Result: Inhibited HepG2 cell migration in a concentration-dependent manner, reducing the wound healing rate from 36.49% (control) to 3.43% at 6 μM.

Cell Invasion Assay[1]

Cell Line: human liver cancer HepG2 cells
Concentration: 2, 4 and 6 μM
Incubation Time: 24 h
Result: Inhibited HepG2 cell invasion in a concentration-dependent manner, reducing the percentage of invasive cells from 100% (control) to 19.85% at 6 μM.

Cell Cycle Analysis[1]

Cell Line: human liver cancer HepG2 cells
Concentration: 2, 4 and 6 μM
Incubation Time: 48 h
Result: Induced concentration-dependent G0/G1 phase arrest: the percentage of cells in G0/G1 phase increased from 65.30% (control) to 79.77% at 6 μM.
Decreased S phase percentage from 24.03% to 13.62% and G2/M phase percentage from 10.67% to 6.61%.

Western Blot Analysis[1]

Cell Line: human liver cancer HepG2 cells
Concentration: 2, 4 and 6 μM
Incubation Time: 48 h
Result: Reduced p-AKT (Ser473) levels in a concentration-dependent manner (P < 0.01) while total AKT levels remained unchanged.
Decreased Bcl-2 expression, increased BAX expression, and elevated cleaved-caspase-3 and cleaved-PARP levels in a concentration-dependent manner.
In Vivo

Compound 17 (AKT1-IN-13) (50-100 mg/kg; i.g.; daily; 14 days) potently inhibits orthotopic hepatocellular carcinoma growth in male C57BL/6 mice via an AKT1-dependent mechanism, reducing average tumor weight by over 56%, while maintaining a favorable safety profile with no impact on body weight[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 3-4 weeks old, 16-18 g, orthotopic liver cancer transplantation model via Hepa1-6 cancer tissue implantation)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: i.g.; daily; 14 days
Result: Reduced average tumor weight to 0.90 g (50 mg/kg group) and 0.86 g (100 mg/kg group) compared to 2.09 g in vehicle control group.
Reduced HCC cell infiltration, disordered arrangement, and multinuclear cell levels in treated groups relative to controls.
Reduced p-AKT levels significantly in both treatment groups compared to controls, with no significant change in total AKT protein levels.
Caused no significant changes in mouse body weight during the study period.
Molecular Weight

793.74

Formula

C43H45BrN4O6
SMILES

COC1=CC(NC2=CC=C(N=C2)Br)=C3C=C1OC4=CC=CC(C[C@H]5C6=C(CCN5C)C=C(C(OC7=C8C(CCN([C@H]8C3)C)=CC(OC)=C7OC)=C6)OC)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AKT1-IN-13 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AKT1-IN-13AktPAKPKAMEKERKApoptosisBcl-2 FamilyCaspasePKBProtein kinase Bp21 activated kinasesProtein kinase AMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesHepG2 cellsPAK1AKT1hepatocellular carcinomacaspase 3BAXMAP2K1MAPK1Bcl-2Inhibitorinhibitorinhibit

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