2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis CDK Caspase PARP
  4. TMLB-C16

TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research.

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

TMLB-C16

TMLB-C16 Chemical Structure

CAS No. : 2923531-50-2

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.

TMLB-C16 Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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

TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research[1].

In Vitro

TMLB-C16 (72 h) demonstrates broad antitumor activities in 13 B3GAT3 high expressed cancer cell lines (such as NCI-H460, NCI-H1650, and Calu3 cells) in a B3GAT3-dependent manner, with IC50 values below 20 μM[1].
TMLB-C16 (0-10 μM, 14 days) prevents colony formation in a dose-dependent manner in MHCC-97H and HCCLM3 cells[1].
TMLB-C16 (0-10 μM, 24 h) inhibits cell migration and inhibits cell division in MHCC-97H and HCCLM3 cells[1].
TMLB-C16 (0-10 μM, 48 h) induces G0/G1-phase cell cycle arrest and apoptosis in MHCC-97H and HCCLM3 cells in a dose-dependent manner, accompanied by enhanced p21, p53, and retinoblastoma-associated protein (Rb) levels and decreased CDK6, cyclin E1, and phosphorylated-Rb (p-Rb) levels[1].

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

TMLB-C16 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MHCC-97H and HCCLM3 cells
Concentration: 0, 5, and 10 μM
Incubation Time: 14 days
Result: Prevented colony formation in a dose-dependent manner.

Cell Migration Assay [1]

Cell Line: MHCC-97H and HCCLM3 cells
Concentration: 0, 5, and 10 μM
Incubation Time: 24 h
Result: Suppressed the wound healing of MHCC-97H and HCCLM3 cells from about 22.22% to 0.86% and 15.71% to 1.90%, respectively.

Cell Cycle Analysis[1]

Cell Line: MHCC-97H and HCCLM3 cells
Concentration: 0, 5, and 10 μM
Incubation Time: 24 h
Result: Remarkably repressed the percentage of S-phase in MHCC-97H and HCCLM3 cells at the concentration of 10 and 5 μM, respectively, by accumulating cells in the G0/G1-phase.

Western Blot Analysis[1]

Cell Line: MHCC-97H and HCCLM3 cells
Concentration: 0, 5, and 10 μM
Incubation Time: 48 h
Result: Induced expression of the epithelial surface marker E-cadherin as well as loss of the mesenchymal markers such as N-cadherin, vimentin, matrix metalloproteinase-2 (MMP-2), MMP-9, and zinc finger E-box-binding homeobox 1 (ZEB1).
Significantly enhanced expression of p21, p53, and Rb, and decreased CDK6, cyclin E1, and p-Rb in a dose-dependent manner.
Remarkably enhanced the expression levels of active c-PARP and c-caspase-3 in MHCC-97H and HCCLM3 cells.

Apoptosis Analysis[1]

Cell Line: MHCC-97H and HCCLM3 cells
Concentration: 0, 5, and 10 μM
Incubation Time: 48 h
Result: Induced apoptosis at both tested concentrations.
Increased the early and late apoptotic rates in MHCC-97H at 5 μM by 8.09% and 6.21%,respectively.
Increased the early and late apoptotic rates in MHCC-97H at 10 μM by 29.93% and 15.77%,respectively.
In Vivo

TMLB-C16 (5, 10 and 20 mg/kg, i.g., daily from day 7 to day 31) inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models[1].

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

Animal Model: Male BALB/c nude mice (6-8 weeks) subcutaneously injected with MHCC-97H and HCCLM3 cells[1]
Dosage: 5, 10 and 20 mg/kg
Administration: i.g., daily from day 7 to day 31
Result: Exhibited a dose-dependent tumor inhibition effect in MHCC-97H xenograft model with 70% and 73.49% tumor growth inhibition at doses of 10 and 20 mg/kg, respectively.
Exhibited a tumor growth inhibition rate of approximately 59% at the dose of 10 mg/kg in HCCLM3 xenograft model.
Molecular Weight

453.88

Formula

C23H20ClN3O5
CAS No.
SMILES

O=C(C1=CC2=C(NC=C2C(C(NC3C(N(CC3)C4=CC=C(C)C=C4Cl)=O)=O)=O)C=C1)OC
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.

TMLB-C16 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:

TMLB-C162923531-50-2ApoptosisCDKCaspasePARPCyclin dependent kinasepoly ADP ribose polymeraseB3GAT3MHCC-97HHCCLM3 cellsxenograft tumor mouse modelhepatocellular carcinomaInhibitorinhibitorinhibit

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:
TMLB-C16
Cat. No.:
HY-177796
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.