Referencia número: HY-184178A

HF-125

Name: HF-125
Brand: MedChemExpress
SKU: HY-184178A
Price: 1025.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.95%
Fòrmula: C₂₄H₂₅ClF₃N₅O₄S
Peso molecular:572.00

Almacenamiento:

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

HF-125 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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.

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.

Chemical Information

Appearance Solid
Peso molecular 572.00
Fòrmula C₂₄H₂₅ClF₃N₅O₄S
Color White to off-white
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7483 mL

8.7413 mL

17.4825 mL

5 mM

0.3497 mL

1.7483 mL

3.4965 mL

10 mM

0.1748 mL

0.8741 mL

1.7483 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Chowdhury SG, et al. HF-I25, a first-in-class computer-modeled novel inhibitor of Tribbles 2, for therapy of enzalutamide resistant, neuroendocrine prostate cancer. bioRxiv. 2026;2026.04.27.720588.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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HF-125