2. Apoptosis
  3. Apoptosis
  4. HF-125

HF-125 is an orally active, highly selective small-molecule inhibitor of Tribbles 2 (TRIB2). HF-125 promotes the destabilization and degradation of TRIB2 protein via the proteasome pathway. HF-125 downregulates neuroendocrine markers, induces cell cycle arrest and apoptosis, inhibits tumor cell colony formation and invasion, and reverses tumor cell resistance to Enzalutamide (HY-70002). HF-125 significantly inhibits tumor growth in SCID mouse xenograft models, and exerts synergistic inhibitory effects when combined with Enzalutamide. HF-125 can be used in research related to prostate cancer.

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

HF-125

HF-125 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.

HF-125 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HF-125 is an orally active, highly selective small-molecule inhibitor of Tribbles 2 (TRIB2). HF-125 promotes the destabilization and degradation of TRIB2 protein via the proteasome pathway. HF-125 downregulates neuroendocrine markers, induces cell cycle arrest and apoptosis, inhibits tumor cell colony formation and invasion, and reverses tumor cell resistance to Enzalutamide (HY-70002). HF-125 significantly inhibits tumor growth in SCID mouse xenograft models, and exerts synergistic inhibitory effects when combined with Enzalutamide. HF-125 can be used in research related to prostate cancer[1].

In Vitro

HF-125 (2-4 μM) induces proteasome-dependent degradation of TRIB2 protein in LN-TRIB2 cells[1].
HF-125 (1-2 μM; 72 h) re-sensitizes LNCaP-ENR, MDA PCa-2b-ENR, LN-TRIB2, and MDA PCa-2b-TRIB2 prostate cancer cells to Enzalutamide (HY-70002)[1].
HF-125 (1 μM; 24 h) enhances Enzalutamide-induced DNA fragmentation and cell death in LNCaP-ENR and MDA PCa-2b-ENR prostate cancer cells[1].
HF-125 (2-8 μM; 72 h) reduces cell viability in LN-Trio2, LN-Trib2, NCI-H660, NCI-H660-01, LASCPC-01, and TRAMP-C1 NEPC cell lines in a dose-dependent manner[1].
HF-125 (2-6 μM; 48 h) downregulates TRIB2 and neuroendocrine marker proteins (N-Myc, EZH2, ASCL1, CGA, ENO2, SYP) while upregulating AR and PSA in LN-TRIB2 cells[1].
HF-125 (2-6 μM; 24 h) induces dose-dependent apoptosis in LN-TRIB2 cells[1].
HF-125 (2-4 μM; 24 h) induces G2M phase cell cycle arrest in LN-TRIB2 cells[1].
HF-125 (2-6 μM; 14 days) reduces the clonogenic potential of LN-TRIB2 cells in a dose-dependent manner[1].
HF-125 (2-6 μM; 16 h) reduces the invasive capacity of LN-TRIB2 cells in a dose-dependent manner[1].
HF-125 (1 μM; 72 h) synergizes with 10 μM enzalutamide to reduce cell viability in LNCaP and MDA PCa-2b prostate cancer cells[1].
HF-125 (1 μM; 16 h) synergizes with 10 μM enzalutamide to inhibit invasion in LNCaP and MDA PCa-2b prostate cancer cells after 16 hours of co-treatment[1].

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

HF-125 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP-ENR, MDA PCa-2b-ENR, LN-TRIB2, MDA PCa-2b-TRIB2 prostate cancer cells
Concentration: 1， 2 μM (combined with 10, 20, 30 μM enzalutamide)
Incubation Time: 72 h
Result: Re-sensitized LNCaP-ENR, MDA PCa-2b-ENR, LN-TRIB2, and MDA PCa-2b-TRIB2 cells to enzalutamide, reducing cell viability significantly compared to enzalutamide treatment alone.

ELISA Assay[1]

Cell Line: LNCaP-ENR, MDA PCa-2b-ENR prostate cancer cells
Concentration: 1 μM (combined with 10-20 μM enzalutamide)
Incubation Time: 24 h
Result: Increased DNA fragmentation in LNCaP-ENR and MDA PCa-2b-ENR cells, indicating enhanced cell death.

Cell Viability Assay[1]

Cell Line: LN-Trio2, LN-Trib2, NCI-H660, NCI-H660-01, LASCPC-01, TRAMP-C1 NEPC cell lines
Concentration: 2, 4, 6, 8 μM
Incubation Time: 72 h
Result: Reduced cell viability in all tested NEPC cell lines in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: LN-TRIB2 cells
Concentration: 2, 4, 6 μM
Incubation Time: 48 h
Result: Downregulated TRIB2, N-Myc, EZH2, ASCL1, CGA, ENO2, and SYP protein levels in a dose-dependent manner, while upregulating AR and PSA protein levels.
At 2 μM, reduced TRIB2, N-Myc, ASCL1, and SYP levels similarly to TRIB2-shRNA knockdown.

Apoptosis Analysis[1]

Cell Line: LN-TRIB2 cells
Concentration: 2, 4, 6 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, with early apoptotic cells increasing from 1.2% to 7.4% (2 μM), 9.3% (4 μM), and 31.1% (6 μM), and late apoptotic cells increasing from 1.4% to 24.0% (2 μM), 24.9% (4 μM), and 15.6% (6 μM).
Total apoptotic cells reached 37.0% at 6 μM.

Cell Cycle Analysis[1]

Cell Line: LN-TRIB2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G2M phase, with G2M population increasing from 12.9% to 19.1% (2 μM) and 12.4% (4 μM), while S phase population decreased from 24.3% to 18.7% (2 μM) and 8.4% (4 μM).

Cell Invasion Assay[1]

Cell Line: LN-TRIB2 cells
Concentration: 2, 4, 6 μM
Incubation Time: 16 h
Result: Reduced cell invasion in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: LN-TRIB2 cells
Concentration: 2, 4, 6 μM
Incubation Time: 14 days
Result: Reduced the clonogenic potential of LN-TRIB2 cells in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line: LNCaP and MDA PCa-2b prostate cancer cells
Concentration: 1 μM (combined with 10 μM enzalutamide)
Incubation Time: 72 h
Result: Synergized with 10 μM enzalutamide to reduce cell viability in both LNCaP and MDA PCa-2b cells.
Combination index (CI) values were <1, and ZIP synergy scores were positive (17.55 for LNCaP, 15.84 for MDA PCa-2b).

Cell Invasion Assay[1]

Cell Line: LNCaP and MDA PCa-2b prostate cancer cells
Concentration: 1 μM (combined with 10 μM enzalutamide)
Incubation Time: 16 h
Result: Synergized with 10 μM enzalutamide to decrease cell invasion in LNCaP cells, with mean invaded cells per field decreasing from ~150 to ~70 (combined treatment).
In Vivo

HF-125 (40 mg/kg; p.o.; daily; 28 days) strongly inhibits enzalutamide-resistant neuroendocrine prostate cancer tumor growth in SCID SHO mice, with significant downregulation of TRIB2 and associated neuroendocrine and proliferation markers, and no overt toxicity[1].

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

Animal Model: SCID SHO (6-week-old male)[1]
Dosage: 40 mg/kg
Administration: p.o.; daily; 28 days
Result: Strongly inhibited ERPC-NE tumor growth, with tumor volumes significantly lower than vehicle controls across all 4 weeks of treatment.
Downregulated protein levels of TRIB2, N-Myc, EZH2, ASCL1, and Ki-67 in tumor tissue compared to vehicle controls.
Caused no overt toxicity to general animal health.
Molecular Weight

572.00

Formula

C24H25ClF3N5O4S
SMILES

CS(C1=C(NC2=NC(NC3=CC=C(C4CCNCC4)C=C3)=NC=C2Cl)C=CC=C1)(=O)=O.O=C(O)C(F)(F)F
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.

HF-125 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:

HF-125HF125HF 125ApoptosisTRIB2proteasome pathwayLNCaP-ENR cellsSCID SHO miceNEPC cell linesapoptosisMDA PCa-2b-TRIB2 cellsLN-TRIB2 cellsenzalutamide-resistant prostate cancer-neuroendocrine cellsMDA PCa-2b-ENR 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:
HF-125
Cat. No.:
HY-184178A
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.