HhAntag
Based on 1 publication(s) in Google Scholar
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
For research use only. We do not sell to patients.
- Purity: 99.40%
- CAS No.: 496794-70-8
- Formula: C24H23ClN4O3
- Molecular Weight:450.92
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HhAntag
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | IC50 |
100 nM
Compound: 2, HhAntag
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Inhibition of Hh signal-induced alkaline phosphatase activity in mouse C3H10T1/2 cells after 4 days
Inhibition of Hh signal-induced alkaline phosphatase activity in mouse C3H10T1/2 cells after 4 days
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[PMID: 20605720] |
| Shh Light II | EC50 |
40 nM
Compound: 96
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Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
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[PMID: 19309080] |
HhAntag (2-30 μM; 72?hours) demonstrates to be?10-times more potent than the natural product SMO antagonist, cyclopamine, at inhibiting Hh pathway activity and it inhibits Hh signalling pathway sensitivitive cells with IC50 values ranging from 2?μM to >30?μM[1].HhAntag inhibits AsPC-1, BXPC-3, CFPAC, HPAC, HPAF-II, KP4, Panc 03.27, PA-TU-8902, PSN-1, SU.86.86 cells with IC50 values of 30 μM, 5.4 μM, 5.8 μM, 2.7 μM, 6.2 μM,10.3 μM, 2.5 μM, 2.9 μM, 5.8 μM and 2.7 μM, respectively[1].HhAntag (100 nM) is needed to completely inhibit Hh signalling in a Hh-responsive human mesenchymal cell line (HEPM) expressing a?GLI?luciferase reporter construct (HEPM-rep), the IC50?of 5?nM 400-times lower than that required to inhibit cell growth by 50% in the most sensitive cancer cell line (1.9?μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Primary human xenografts in female CD1 nu/nu mice of 6–8 weeks (DLD-1, HT55 and HT-29 cells)[1]
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Dosage:75 mg/kg or 100 mg/kg
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Administration:Oral administraion; twice daily; 25 days
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Result:Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts.
Chemical Information
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CAS No. 496794-70-8
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Appearance Solid
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Molecular Weight 450.92
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Formula C24H23ClN4O3
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(Cl)C(C2=NC3=CC=C(N(C)C)C=C3N2)=C1)C4=CC(OC)=CC(OC)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Signal
2025 Apr 15:132:111807. PMID: 40239727
Solvent & Solubility
DMSO : ≥ 100 mg/mL (221.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 3 mg/mL (6.65 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2177 mL | 11.0884 mL | 22.1769 mL | 55.4422 mL |
| 5 mM | 0.4435 mL | 2.2177 mL | 4.4354 mL | 11.0884 mL | |
| 10 mM | 0.2218 mL | 1.1088 mL | 2.2177 mL | 5.5442 mL | |
| 15 mM | 0.1478 mL | 0.7392 mL | 1.4785 mL | 3.6961 mL | |
| 20 mM | 0.1109 mL | 0.5544 mL | 1.1088 mL | 2.7721 mL | |
| 25 mM | 0.0887 mL | 0.4435 mL | 0.8871 mL | 2.2177 mL | |
| 30 mM | 0.0739 mL | 0.3696 mL | 0.7392 mL | 1.8481 mL | |
| 40 mM | 0.0554 mL | 0.2772 mL | 0.5544 mL | 1.3861 mL | |
| 50 mM | 0.0444 mL | 0.2218 mL | 0.4435 mL | 1.1088 mL | |
| 60 mM | 0.0370 mL | 0.1848 mL | 0.3696 mL | 0.9240 mL | |
| 80 mM | 0.0277 mL | 0.1386 mL | 0.2772 mL | 0.6930 mL | |
| 100 mM | 0.0222 mL | 0.1109 mL | 0.2218 mL | 0.5544 mL |
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