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.
- Formula: C24H25ClF3N5O4S
- Molecular Weight:572.00
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
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.
-
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.
-
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 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.
-
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.
-
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 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 Line:LN-TRIB2 cells
-
Concentration:2, 4, 6 μM
-
Incubation Time:16 h
-
Result:Reduced cell invasion in a dose-dependent manner.
-
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 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 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).
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.
Chemical Information
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HF-125 Related Classifications
HY-184178A Related Classifications
Powered by Bioz