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

MS102 是一种口服有效的泛素特异性肽酶 2 (USP2) 抑制剂,其 IC50 为 5.46 μM。MS102 对 ACE2 依赖性冠状病毒具有有效的抗病毒活性。MS102 在体外和体内均能显著降低 V 结构域免疫球蛋白 T 细胞活化抑制因子 (VISTA) 蛋白的丰度。MS102 可用于 SARS-CoV-2 的研究。MS102 可与抗 PD-1 免疫方法联合使用以增强抗肿瘤免疫反应。

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MS102

MS102 Chemical Structure

CAS No. : 3058587-77-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

MS102 (4-10 μM;24-48 h) 在阻断原代人支气管上皮细胞 (NHBE) 感染 SARS-CoV-2 野生型病毒方面也表现出更高的效果。MS102 在 HepG2 和 Calu-3 细胞中具有极低的细胞毒性[1]
MS102 能有效抑制 ACE2 依赖性冠状病毒 hCoV-NL63 (一种 ACE2 依赖性冠状病毒),其 EC50 值为 80 nM[1]
MS102 在 MDA-MB-231、SUM159、MDA-MB-436、EMT6 和 RENCA 细胞中表现出 VISTA 蛋白水平的显著降低[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MS102 (25 mg/kg,腹腔注射,一天一次,连续 4 天) 在 K102- hACE2 转基因小鼠中降低 SARS-CoV-2 病毒载量和肺部病理变化 [1]
MS102 (10 mg/kg,每日腹腔注射,共 21 天) 通过减少 VISTA 并促进 T 细胞活性,在同源肿瘤小鼠模型中增强抗-PD-1 免疫治疗[2]

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.
分子量

596.44

Formula

C24H17BrF3N3O3S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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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