2. PI3K/Akt/mTOR Apoptosis Epigenetics Cell Cycle/DNA Damage Stem Cell/Wnt
  3. Akt Apoptosis Caspase PARP β-catenin
  4. AKT-IN-28

AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells.

For research use only. We do not sell to patients.

AKT-IN-28 Chemical Structure

AKT-IN-28 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

AKT-IN-28 Related Antibodies

Top Publications Citing Use of Products

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All Caspase Isoform Specific Products:

View All Isoforms
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

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells[1].

IC50 & Target

Caspase 3

 

PARP

 

Akt

2.07 μM (Kd)

In Vitro

AKT-IN-28 (Compound L8) has a potent anti-proliferative activity (IC50 s of 4.51, 4.57, 5.07, 8.94 and 6.59 μM for HCT-8, HCT-116, PC-3, MDA-MB-231, and HeLa cells, respectively), with low cytotoxicity in normal cells (IC50 s of > 100  and 67 μM for MCF-10A and HCoEpiC cells)[1].
AKT-IN-28 (1-4 μM, 24 h) dose-dependently decreases the Akt enzyme activity, and significantly inhibits the total Akt, p-Akt, PARP and β-catenin protein expression, cell proliferation activity and migration, while increase of cleaved-PARP protein level in HCT-8 and HCT-116 cells[1].
AKT-IN-28 (0.25-1 μM, 7 days) significantly inhibites the viability of colon cancer cells with reduction of colony formation of HCT-116 cells[1].
AKT-IN-28 (2-8 μM, 24 h) effectively induces cell apoptosis and arrests cell cycle in G2/M phase (8 μM) with decrease of cycle-related proteins CDH1, CDK1, and CDC20, and increases caspase3 activity in HCT-116 and HCT-8 cells[1].
AKT-IN-28 (2-8 μM, 2-24 h) significantly reduces the glucose consumption, lactate production, and ATP level in HCT-116 cells[1].

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

AKT-IN-28 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly reduced the percentage of EdU-positive cells.

Cell Migration Assay [1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 3, 6, 12, 24 h
Result: Significantly reduced the number of metastasis colon cancer cells and enlarged the space area of migrating cells.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly inhibited the total Akt, p-Akt, PARP and β-catenin protein expression but increased cleaved-PARP protein level.
Obviously decreased the expression levels of cycle-related proteins CDH1, CDK1, and CDC20.

Cell Cycle Analysis[1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h
Result: Arrested the cell cycle at G2/M phase at 8 μM in HCT-8 and HCT-116 cells.

Apoptosis Analysis[1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h
Result: Effectively induced cell apoptosis in HCT-8 and HCT-116 cells.
Molecular Weight

573.57

Formula

C32H28FNO8
SMILES

OC1=CC=C(O)C2=C1C(C=C(C(OC(CC3=CC=C(NC(COC4=CC=C(F)C=C4)=O)C=C3)=O)C/C=C(C)\C)C2=O)=O
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

AKT-IN-28 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

AKT-IN-28AktApoptosisCaspasePARPβ-cateninPKBProtein kinase Bpoly ADP ribose polymerase Beta cateninAllosteric inhibitorAnticancerShikoninHCT-8 cellsHCT-116 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AKT-IN-28
Cat. No.:
HY-174254
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.