2. PI3K/Akt/mTOR Epigenetics Apoptosis
  3. Akt PI3K Epigenetic Reader Domain c-Myc
  4. LCI40

LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma.

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

LCI40

LCI40 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.

LCI40 Related Antibodies

Top Publications Citing Use of Products

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All PI3K Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma[1].

IC50 & Target[1]

BRD4 (BD2)

1.88 μM (IC50)

BRD4 (BD1)

0.19 μM (IC50)

PI3Kγ

0.66 μM (IC50)

PI3Kα

0.071 μM (IC50)

PI3Kβ

0.17 μM (IC50)

In Vitro

LCI40 (1.0 μM) is highly selective for PI3K family enzymes and PIK3CA mutants[1].
LCI40 (1.0 μM) is highly selective for BET family bromodomains, particularly the BD1 domains of BRD4, BRD3, BRD2, and BRDT[1].
LCI40 (48 h) potently reduces cell viability in human Mino (IC50 = 357 nM) and JeKo-1 (IC50 = 519 nM) mantle cell lymphoma cell lines[1].
LCI40 (0.1-1 μM; 2 h) dose-dependently inhibits PI3K/AKT signaling (pAKTS473) and reduces c-MYC protein expression in IgM-stimulated human Mino mantle cell lymphoma cells[1].
LCI40 (0.5 μM; 48 h) interferes with IL-4-mediated alternative macrophage activation in mouse BMDMs by suppressing M2 marker expression and metabolic reprogramming[1].
LCI40 (0.1-5 μM; 1 h pretreatment) dose-dependently restrains CD3/CD28-mediated mouse pan-T cell activation and proliferation, reduces activation marker and effector gene expression, and has micromolar cytotoxicity to resting T cells[1].

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

LCI40 Related Antibodies

Western Blot Analysis[1]

Cell Line: IgM-stimulated human Mino mantle cell lymphoma cells
Concentration: 0.1; 0.5; 1 μM
Incubation Time: 2 h
Result: Dose-dependently inhibited phosphorylation of AKT at S473.
Reduced c-MYC protein levels.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-last AUC0-∞ Vz/F CL/F
Mice[1] 20 mg/kg p.o. 2.5 h 0.3 h 336.5 ng/mL 153.7 ng·h/mL 159.2 ng·h/mL 472.6 L/kg 128.1 L/h/kg
Molecular Weight

388.42

Formula

C23H20N2O4
SMILES

O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC(C(OC)=CC=N5)=C5C=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
  • 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.

LCI40 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:

LCI40LCI 40LCI-40AktPI3KEpigenetic Reader Domainc-MycPKBProtein kinase BPhosphoinositide 3-kinaseMycPI3KδMinomantle cell lymphomaBRD4PI3KαPI3KγPI3KβPIK3CAJeKo-1Inhibitorinhibitorinhibit

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:
LCI40
Cat. No.:
HY-183770
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.