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.
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- CAS No.: 3058587-77-9
- Formule: C24H17BrF3N3O3S2
- Masse moléculaire:596.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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USP2 5.46 μM (IC50) |
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.
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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Masse moléculaire 596.44
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)