2. Stem Cell/Wnt Apoptosis
  3. YAP Apoptosis
  4. LC-TD-05

LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC50 values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC50 of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma.

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

LC-TD-05

LC-TD-05 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.

LC-TD-05 Related Antibodies

Top Publications Citing Use of Products

View All YAP Isoform Specific Products:

View All Isoforms
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC50 values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC50 of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma[1].

IC50 & Target[1]

TEAD4

68.3 nM (IC50)

TEAD1

116.6 nM (IC50)

TEAD2

168.7 nM (IC50)

TEAD3

1261.0 nM (IC50)

In Vitro

LC-TD-05 (72 h) selectively inhibits the proliferation of HCC LM3, SK-HEP-1, HepG2 and Huh7 cells, with IC50 values of 248 nM, 964 nM, 7.108 μM and 4.603 μM, respectively. It exhibits extremely low cytotoxicity toward non-tumorigenic HEK293T and THLE-2 cells[1].
LC-TD-05 (3 μM; 10-14 d) potently inhibits colony formation of HCC LM3 cells[1].
LC-TD-05 (0.3-10 μM; 3 h) downregulates the mRNA expression of TEAD target genes CTGF and CYR61 in HCC LM3 cells in a dose-dependent manner[1].
LC-TD-05 (3-10 μM; 72 h) dose-dependently induces apoptosis in hepatocellular carcinoma LM3 cells[1].
LC-TD-05 inhibits TEAD-associated transcriptional programs in HCC LM3 cells, including downregulation of cell cycle progression genes and canonical TEAD target genes[1].

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

LC-TD-05 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCC LM3 cells
Concentration: 3 μM
Incubation Time: 10-14 days
Result: Significantly reduced the number of colonies formed by HCC LM3 cells compared to DMSO control.

Real Time qPCR[1]

Cell Line: HCC LM3 cells
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 3 hours
Result: Significantly downregulated the mRNA expression of CTGF and CYR61 in a dose-dependent manner, with maximal suppression at 10 μM.

Apoptosis Analysis[1]

Cell Line: HCC LM3 cells
Concentration: 3 and 10 μM
Incubation Time: 72 hours
Result: Induced a dose-dependent increase in the proportion of apoptotic HCC LM3 cells, with significant elevation at 3 μM and 10 μM compared to DMSO control.
Parmacokinetics
Species Dose Route Cmax AUC0-∞ CL MRT0-∞ T1/2 Tmax F
Rat[1] 1 mg/kg i.v. 667 ng/mL 2536 ng·h/mL 467 mL/h/kg 6.99 h 5.60 h / /
Rat[1] 10 mg/kg p.o. 1313 ng/mL 13616 ng·h/mL / 7.46 h 5.54 h 2.00 h 53.7 %
In Vivo

LC-TD-05 (50 mg/kg; i.p.; once daily; for 17 consecutive days) exhibits significant in vivo anti-tumor activity in the HCC LM3 xenograft model[1].

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

Animal Model: BALB/c nude (male, 4-6 weeks old)[1]
Dosage: 50 mg/kg
Administration: i.p.; once daily; 17 days
Result: Achieved a tumor growth inhibition (TGI) of 75%.
Markedly reduced tumor weights compared to vehicle controls.
Showed no significant change in body weight relative to the vehicle group.
Reduced protein and transcript levels of the TEAD target genes CTGF and CYR61 in treated tumor tissues.
Molecular Weight

492.49

Formula

C27H23F3N4O2
SMILES

O=C(N1CCN(C(C2=CC=CC3=C2C=CN3C4=CC=C(C(F)(F)F)C=C4)=O)CC1)NC5=CC=CC=C5
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.

LC-TD-05 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:

LC-TD-05YAPApoptosisYes-associated proteinHuh7 cellsSK-HEP-1 cellsHEK293T cellshepatocellular carcinomaHepG2 cellsTEAD2TEAD4TEAD1TEAD3HCC LM3 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:
LC-TD-05
Cat. No.:
HY-183753
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.