2. PI3K/Akt/mTOR Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Akt Microtubule/Tubulin Apoptosis
  4. AKT1-IN-11

AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer.

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AKT1-IN-11

AKT1-IN-11 Chemical Structure

CAS No. : 3087064-94-3

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AKT1-IN-11 Related Antibodies

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Description

AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer[1].

In Vitro

AKT1-IN-11 (Compound 2b) (48 h) inhibits HCT-116, HT-29, HCT-8 and NCM460 cell proliferation with IC50 values of 0.77, 0.48, 1.68 and 52.28 μM[1].
AKT1-IN-11 (0.2 μM, 12-24 h) induces apoptosis in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM; 24 h) inhibits cell migration and reverses the epithelial mesenchymal transition process in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM; 2-8 h) induces G2/M phase arrest in HCT-116 cells, and downregulates the expression of Cyclin B1 and CDK4[1].
AKT1-IN-11 (0.1 μM; 12 h) promotes microtubule depolymerization in HCT-116 cells[1].
AKT1-IN-11 (0.1-0.2 μM, 24 h) concentration-dependently downregulates p-AKT expression in HCT-116 cells and inhibits AKT pathway activation[1].

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

AKT1-IN-11 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.1, 0.2 μM
Incubation Time: 2, 4, 8 and 24 h
Result: Downregulated the expression of phosphorylated AKT1 (p-AKT) in a concentration-dependent manner.
Downregulated the expression of Cyclin B1 and CDK4.
Reduced the levels of E-cadherin and increased the levels of N-cadherin.

Immunofluorescence[1]

Cell Line: HCT-116 cells
Concentration: 0.1 μM
Incubation Time: 12 h
Result: Disrupted microtubule structure.
In Vivo

AKT1-IN-11(Compound 2b) (1-2 mg/kg; i.p.; once every two days; 6 doses) inhibits tumor growth in HCT-116 xenograft mice models[1].

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

Animal Model: Mice (Male, BALB/c-nu/nu, 6-8 weeks) with subcutaneous injection of HCT-116 cells[1]
Dosage: 1, 2 mg/kg
Administration: Intraperitoneally injection; once every two days; 6 doses
Result: Reduced tumor volumes without causing a significant decrease in body weight.
Reduced the tumor weight-to-body weight ratio.
Reduced the Ki67-positive rate and increased the TUNEL-positive rate.
Molecular Weight

692.69

Formula

C33H32N4O11S
CAS No.
SMILES

COC1=C(OC)C(OC)=CC([C@H]2[C@]3([H])[C@@](COC3=O)([H])[C@@H](OCC4=CN(S(C5=CC=C(NC(C)=O)C=C5)(=O)=O)N=N4)C6=CC7=C(OCO7)C=C26)=C1
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References
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AKT1-IN-11 Related Classifications

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Keywords:

AKT1-IN-113087064-94-3AktMicrotubule/TubulinApoptosisPKBProtein kinase Bcolorectal cancerderivativesAKTHCT-116HT-29HCT-8NCM460Inhibitorinhibitorinhibit

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