1. Cell Cycle/DNA Damage Anti-infection Immunology/Inflammation
  2. Deubiquitinase SARS-CoV VISTA
  3. 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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MS102

MS102 Chemical Structure

CAS No. : 3058587-77-9

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Description

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[1][2].

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 (25 mg/kg, i.p., daily for 4 days, followed by 6 hours challenge with SARS-CoV-2 WT) reduces SARS-CoV-2 viral load and lung pathology in K18-hACE2 transgenic mice[1].
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.

Animal Model: K18-hACE2 (transgenic mice, human ACE2 driven by K18 promoter) were infected with SARS-CoV-2 Omicron BA.2 sublineage[1]
Dosage: 25 mg/kg
Administration: Daily for 4 days, followed by 6 h challenge with SARS-CoV-2 WT
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. 
Animal Model: Femal BALB/c (6-week-old) were subcutaneously injected with 1 × 105 MC38 cells[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal, daily, for 21 days
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.
Molecular Weight

596.44

Formula

C24H17BrF3N3O3S2

CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MS102
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HY-179630
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