2. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. PI3K HDAC Bcl-2 Family Caspase Reactive Oxygen Species (ROS)
  4. PI3Kδ/HDAC6-IN-1

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3.

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

PI3Kδ/HDAC6-IN-1 Chemical Structure

PI3Kδ/HDAC6-IN-1 Chemical Structure

CAS No. : 3075011-99-0

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.

PI3Kδ/HDAC6-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3[1].

IC50 & Target

PI3Kδ

2.4 nM (IC50)

HDAC6

6.2 nM (IC50)

In Vitro

PI3Kδ/HDAC6-IN-1 (compound 22E) (0.1 nM -10 μM, 24-120 h) shows inhibitory activity against both PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.4 nM, and exhibits antiproliferative activity against JEKO-1 cells[1].

PI3Kδ/HDAC6-IN-1 (10-30 μM, 45 °C-85 °C) improves thermal stability of PI3Kδ and HDAC6[1].

PI3Kδ/HDAC6-IN-1 (0.1-10 μM, 4 days) inhibits the proliferation of NHL cells, with IC50 values of 34 nM (SU-DHL-6 cells) and 53 nM (JEKO-1 cells)[1].

PI3Kδ/HDAC6-IN-1 (0.3-9 μM, 24 h) induces G0/G1 phase arrest in the SU-DHL-6 and JEKO-1 cells[1].

PI3Kδ/HDAC6-IN-1 (0.3-9 μM, 72 h) induces apoptosis (Annexin V positive) concentration-dependent in the SU-DHL-6 and JEKO-1 cells[1].

PI3Kδ/HDAC6-IN-1 (0.3-9 μM, 12 h) inhibits PI3K and HDAC-related proteins at the cellular level in the SU-DHL-6 and JEKO-1 cells[1].

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

PI3Kδ/HDAC6-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 24 h
Result: Increased the ratio of cells in G0/G1 phase, blocked cancer cells in the G0/G1 phase.
Downregulated cyclin D1, cyclin E1, CDK6, CDK4, and CDK2 proteins.

Apoptosis Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 72 h
Result: Induced Annexin V positivity, downregulated the anti-apoptotic protein BCL-2, increased levels of cleaved PARP and cleaved caspase-3.
Induced a concentration-dependent increase in the ROS-positive cell count in JEKO-1 cells.

Western Blot Analysis[1]

Cell Line: SU-DHL-6 and JEKO-1 cells
Concentration: 0.3 μM, 1 μM, 3 μM, 9 μM
Incubation Time: 12 h
Result: Inhibited hosphorylation of downstream signaling proteins of PI3K, including AKT, P70S6K, and 4EBP1, as well as the oncogene-encoded protein c-MYC, while having no effect on total protein levels.
Increased histone H3 and α-tubulin acetylation levels.
In Vivo

PI3Kδ/HDAC6-IN-1 (compound 22E) (25 mg/kg, p.o., once a day, 21 days) has anti-tumor potential, inhibits PI3K pathway and HDAC-related proteins in SU-DHL-6 and JEKO-1 tumor xenograft models in NOD-SCID mice[1].

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

Animal Model: SU-DHL-6 and JEKO-1 tumor xenograft models in NOD-SCID mice[1]
Dosage: 25 mg/kg
Administration: p.o., 21 days
Result: Reduced tumor growth, exhibited antitumor activity, with corresponding TGI rates of 69.42 % in the SU-DHL-6 model and 67.56 % in the JEKO-1 model.
Reduced p-AKT levels and increased acetyl-α-tubulin levels, reduced Ki-67 levels and increased cleaved caspase-3 levels.
Molecular Weight

650.73

Formula

C34H38N10O4
CAS No.
SMILES

CCC(N1C2=NC(N(C)C(CN3C(CN(CC4=CC=C(/C=C/C(NO)=O)C=C4)CC3)=O)=N5)=C5C(N6CCOCC6)=N2)=NC7=C1C=CC=C7
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.

PI3Kδ/HDAC6-IN-1 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:

PI3Kδ/HDAC6-IN-13075011-99-0PI3KHDACBcl-2 FamilyCaspaseReactive Oxygen Species (ROS)Phosphoinositide 3-kinaseHistone deacetylasesInhibitorSU-DHL-6 cellsJEKO-1 cellsapoptosisSU-DHL-6 and JEKO-1 tumor xenograft modelsinhibitorinhibit

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:
PI3Kδ/HDAC6-IN-1
Cat. No.:
HY-174396
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.