HF-125
Based on 1 Customer Validation
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.
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- Purity: 99.95%
- 화학식: C24H25ClF3N5O4S
- 분자량:572.00
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보관:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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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.
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Cell Line:LNCaP-ENR, MDA PCa-2b-ENR, LN-TRIB2, MDA PCa-2b-TRIB2 prostate cancer cells
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Concentration:1， 2 μM (combined with 10, 20, 30 μM enzalutamide)
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Incubation Time:72 h
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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.
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Cell Line:LNCaP-ENR, MDA PCa-2b-ENR prostate cancer cells
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Concentration:1 μM (combined with 10-20 μM enzalutamide)
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Incubation Time:24 h
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Result:Increased DNA fragmentation in LNCaP-ENR and MDA PCa-2b-ENR cells, indicating enhanced cell death.
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Cell Line:LN-Trio2, LN-Trib2, NCI-H660, NCI-H660-01, LASCPC-01, TRAMP-C1 NEPC cell lines
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Concentration:2, 4, 6, 8 μM
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Incubation Time:72 h
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Result:Reduced cell viability in all tested NEPC cell lines in a dose-dependent manner.
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Cell Line:LN-TRIB2 cells
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Concentration:2, 4, 6 μM
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Incubation Time:48 h
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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.
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Cell Line:LN-TRIB2 cells
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Concentration:2, 4, 6 μM
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Incubation Time:24 h
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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.
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Cell Line:LN-TRIB2 cells
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Concentration:2, 4 μM
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Incubation Time:24 h
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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).
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Cell Line:LN-TRIB2 cells
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Concentration:2, 4, 6 μM
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Incubation Time:16 h
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Result:Reduced cell invasion in a dose-dependent manner.
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Cell Line:LN-TRIB2 cells
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Concentration:2, 4, 6 μM
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Incubation Time:14 days
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Result:Reduced the clonogenic potential of LN-TRIB2 cells in a dose-dependent manner.
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Cell Line:LNCaP and MDA PCa-2b prostate cancer cells
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Concentration:1 μM (combined with 10 μM enzalutamide)
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Incubation Time:72 h
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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).
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Cell Line:LNCaP and MDA PCa-2b prostate cancer cells
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Concentration:1 μM (combined with 10 μM enzalutamide)
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Incubation Time:16 h
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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.
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Animal Model:SCID SHO (6-week-old male)[1]
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Dosage:40 mg/kg
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Administration:p.o.; daily; 28 days
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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
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Appearance Solid
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분자량 572.00
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화학식 C24H25ClF3N5O4S
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Color White to off-white
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
용액&용해도
DMSO : 100 mg/mL (174.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7483 mL | 8.7413 mL | 17.4825 mL | 43.7063 mL |
| 5 mM | 0.3497 mL | 1.7483 mL | 3.4965 mL | 8.7413 mL | |
| 10 mM | 0.1748 mL | 0.8741 mL | 1.7483 mL | 4.3706 mL | |
| 15 mM | 0.1166 mL | 0.5828 mL | 1.1655 mL | 2.9138 mL | |
| 20 mM | 0.0874 mL | 0.4371 mL | 0.8741 mL | 2.1853 mL | |
| 25 mM | 0.0699 mL | 0.3497 mL | 0.6993 mL | 1.7483 mL | |
| 30 mM | 0.0583 mL | 0.2914 mL | 0.5828 mL | 1.4569 mL | |
| 40 mM | 0.0437 mL | 0.2185 mL | 0.4371 mL | 1.0927 mL | |
| 50 mM | 0.0350 mL | 0.1748 mL | 0.3497 mL | 0.8741 mL | |
| 60 mM | 0.0291 mL | 0.1457 mL | 0.2914 mL | 0.7284 mL | |
| 80 mM | 0.0219 mL | 0.1093 mL | 0.2185 mL | 0.5463 mL | |
| 100 mM | 0.0175 mL | 0.0874 mL | 0.1748 mL | 0.4371 mL |
HF-125 Related Classifications
HY-184178A Related Classifications
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