MS102
MS102 is an orally active ubiquitin specific peptidase 2 (USP2) inhibitor with an IC50 of 5.46 μM. MS102 has viable antiviral activity against ACE2-dependent coronaviruses. MS102 significantly reduces V-domain Ig suppressor of T cell activation (VISTA) protein abundance in vitro and in vivo. MS102 can be used for the study of SARS-CoV-2. MS102 can be used in combination with anti-PD-1 immunotherapy to enhance the anti-tumor immune response.
For research use only. We do not sell to patients.
- CAS No.: 3058587-77-9
- Formula: C24H17BrF3N3O3S2
- Molecular Weight:596.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
USP2 5.46 μM (IC50) |
In Vitro
MS102 (4-10 μM; 24-48 h) demonstrates improved efficacy in blocking the infection of primary human bronchial epithelial (NHBE) cells by the authentic SARS-CoV-2 wild-type. MS102 has minimal cytotoxicity in HepG2 and Calu-3 cells[1].
MS102 is effective in inhibiting the ACE2-dependent coronavirus hCoV-NL63 (an ACE2-dependent coronavirus) with an EC50 of 80 nM[1].
MS102 demonstrates significant reduction in VISTA protein levels in MDA-MB-231, SUM159, MDA-MB-436, EMT6, and RENCA cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MS102 (10 mg/kg, intraperitoneal daily, for 21 dyas) enhances anti-PD-1 immunotherapy by reducing VISTA and promoting T cell activity in syngeneic mouse tumor models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:K18-hACE2 (transgenic mice, human ACE2 driven by K18 promoter) were infected with SARS-CoV-2 Omicron BA.2 sublineage[1]
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Dosage:25 mg/kg
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Administration:Daily for 4 days, followed by 6 h challenge with SARS-CoV-2 WT
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Result:Showed the enhanced reduction in the 50% tissue culture infectious dose (TCID50) and improved lung pathology in the treated mice.
Exhibited notably enhanced outcomes compared with the control mice.
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Animal Model:Femal BALB/c (6-week-old) were subcutaneously injected with 1 × 105 MC38 cells[2]
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Dosage:10 mg/kg
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Administration:Intraperitoneal, daily, for 21 days
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Result:Significantly reduced VISTA protein levels in tumor tissues, enhanced T cell infiltration, and improved anti-PD-1 immunotherapy efficacy.
Combination therapy with anti-PD-1 led to significant tumor growth inhibition, with survival rates comparable to Vsir KO tumor models.
Chemical Information
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CAS No. 3058587-77-9
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Molecular Weight 596.44
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Formula C24H17BrF3N3O3S2
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SMILES
O=C(NC1=NC(C2=CC=C(Br)C=C2)=CS1)C3=CC(C(F)(F)F)=CC=C3NS(=O)(C4=CC=C(C)C=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (167.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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
References
[1]. Dang F, et al. USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice. Sci Transl Med. 2023;15(725):eadh7668. [Content Brief]
[2]. Li Chen, et al. Targeted destruction of VISTA boosts anti-tumor immunotherapy. Cell Res. 2025 Dec;35(12):987-1002. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6766 mL | 8.3831 mL | 16.7661 mL | 41.9154 mL |
| 5 mM | 0.3353 mL | 1.6766 mL | 3.3532 mL | 8.3831 mL | |
| 10 mM | 0.1677 mL | 0.8383 mL | 1.6766 mL | 4.1915 mL | |
| 15 mM | 0.1118 mL | 0.5589 mL | 1.1177 mL | 2.7944 mL | |
| 20 mM | 0.0838 mL | 0.4192 mL | 0.8383 mL | 2.0958 mL | |
| 25 mM | 0.0671 mL | 0.3353 mL | 0.6706 mL | 1.6766 mL | |
| 30 mM | 0.0559 mL | 0.2794 mL | 0.5589 mL | 1.3972 mL | |
| 40 mM | 0.0419 mL | 0.2096 mL | 0.4192 mL | 1.0479 mL | |
| 50 mM | 0.0335 mL | 0.1677 mL | 0.3353 mL | 0.8383 mL | |
| 60 mM | 0.0279 mL | 0.1397 mL | 0.2794 mL | 0.6986 mL | |
| 80 mM | 0.0210 mL | 0.1048 mL | 0.2096 mL | 0.5239 mL | |
| 100 mM | 0.0168 mL | 0.0838 mL | 0.1677 mL | 0.4192 mL |