M351-0056
Based on 1 Customer Validation
M351-0056 is an orally active VISTA agonist with a Kd value of 12.60 μM. M351-0056 inhibits the activation of the JAK2-STAT2 pathway, reduces the phosphorylation levels of JAK2 and STAT2, and regulates type I interferon (IFN-I) and non-canonical NF-κB pathways. M351-0056 decreases the levels of cytokines (IFN-γ, IL-17A, TNF-α, IL-2 and IL-1β). M351-0056 improves imiquimod (HY-B0180)-induced psoriasis-like skin inflammation, reduces autoantibody levels, kidney damage and immune cell expansion in mice susceptible to chronic graft-versus-host disease and lupus, and delays the progression of systemic lupus erythematosus. M351-0056 can be used in research related to psoriasis-like dermatitis and systemic lupus erythematosus.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.48%
- CAS 番号: 1189495-81-5
- 分子式: C15H12BrFN2O2S3
- 分子量:447.37
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
JAK2 |
STAT2 |
IL-17A |
IL-2 |
IL-1β |
体外実験
M351-0056 inhibits cytokine production in Jurkat cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, 8 weeks old, psoriasis induced by daily topical application of 5% imiquimod cream for 6 days)[1]
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Dosage:25 mg/kg
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Administration:p.o.; daily; 6 days
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Result:Reduced imiquimod-induced ear thickness relative to the model group.
Decreased ear acanthosis from 16 μm to 10 μm.
Reduced back acanthosis from 19 μm to 13 μm.
Significantly decreased serum IFN-γ levels from ~310 pg/mL to ~180 pg/mL.
Significantly decreased serum TNF-α levels from ~25 pg/mL to ~8 pg/mL.
Significantly decreased serum IL-17A levels from ~6.5 pg/mL to ~5.5 pg/mL.
Significantly decreased serum IL-1β levels from ~19 pg/mL to ~7 pg/mL.
Reduced skin tissue protein levels of IFN-γ, TNF-α, IL-1β, IL-17, and IL-23 relative to the model group.
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Animal Model:CB6F1 (female; chronic graft-versus-host disease model)[2]
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Dosage:50 mg/kg/day
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Administration:i.g.; daily; 28 days
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Result:Significantly reduced splenomegaly.
Decreased levels of urinary protein, serum creatinine (CRE), blood urea nitrogen (BUN), anti-double-stranded DNA (anti-dsDNA) antibodies, and total immunoglobulin G (IgG).
Improved renal histopathology (reduced amyloid deposition, glomerular basement membrane/mesangium hyperplasia, and inflammatory cell infiltration).
Reduced immune complex IgG deposition in renal tubules and glomeruli.
Decreased renal expression of interferon-stimulated genes (ISGs) and noncanonical nuclear factor-κB (NF-κB)-related genes.
Reduced phosphorylation of JAK1, STAT1, STAT3, and NF-κB2 p52 proteins in kidney tissue.
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Animal Model:MRL/MpJ-Faslpr/J (MRL/lpr) (female; 12-week-old; spontaneous SLE model with recessive Fas gene mutation)[2]
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Dosage:50 mg/kg/day
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Administration:i.g.; daily; 42 days
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Result:Significantly reduced enlargement of spleen, kidney, thymus, and mesenteric lymph nodes.
Decreased levels of urinary protein/creatinine ratio, serum CRE, BUN, anti-dsDNA antibodies, and total IgG.
Improved renal histopathology (reduced inflammatory cell infiltration, amyloid formation, and glomerular damage).
Reduced immune complex IgG deposition in kidney tissue.
Decreased splenic proportions of plasmacytoid dendritic cells (pDC), neutrophils, mononuclear myeloid-derived suppressor cells (M-MDSC), CD4+ T cells, and CD8+ T cells.
Reduced activation markers (CD44 on CD4+ T cells, MHC-II on M-MDSC).
Decreased renal expression of ISGs and noncanonical NF-κB-related genes.
Reduced phosphorylation of JAK1, STAT3, and NF-κB2 p52 proteins in kidney tissue.
- Kinase activity and phosphorylation assays
- Western Blot
- Imiquimod-Induced Psoriasiform Dermatitis
- TPA/Croton Oil Ear Edema and Dermatitis
- Contact Hypersensitivity Dermatitis
- Protocol for Kinase activity and phosphorylation assays
- Research Protocol for Inflammation-related Diseases
- Pyroptosis Solutions
化学情報
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CAS 番号 1189495-81-5
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性状 Solid
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分子量 447.37
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分子式 C15H12BrFN2O2S3
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Color White to off-white
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SMILES
O=S(NC1=CC=C(C=C1F)Br)(C2=C(C)SC(C3=CSC(C)=N3)=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (223.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hu X, et al. M351-0056 is a novel low MW compound modulating the actions of the immune-checkpoint protein VISTA. Br J Pharmacol. 2021 Mar;178(6):1445-1458. [Content Brief]
[2]. Yang L, et al. Imatinib and M351-0056 enhance the function of VISTA and ameliorate the development of SLE via IFN-I and noncanonical NF-κB pathway. Cell biology and toxicology. 2023 Dec;39(6):3287-3304. [Content Brief]
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Topics Immune Checkpoint: A Critical Target In Tumor Therapy
Immune checkpoints are inhibitory or costimulatory pathways that regulate T-cell activation, peripheral tolerance, and antitumor immune responses, and tumors can exploit these pathways to restrict effector T-cell function and establish immune escape.
2026-06-18
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2353 mL | 11.1764 mL | 22.3529 mL | 55.8822 mL |
| 5 mM | 0.4471 mL | 2.2353 mL | 4.4706 mL | 11.1764 mL | |
| 10 mM | 0.2235 mL | 1.1176 mL | 2.2353 mL | 5.5882 mL | |
| 15 mM | 0.1490 mL | 0.7451 mL | 1.4902 mL | 3.7255 mL | |
| 20 mM | 0.1118 mL | 0.5588 mL | 1.1176 mL | 2.7941 mL | |
| 25 mM | 0.0894 mL | 0.4471 mL | 0.8941 mL | 2.2353 mL | |
| 30 mM | 0.0745 mL | 0.3725 mL | 0.7451 mL | 1.8627 mL | |
| 40 mM | 0.0559 mL | 0.2794 mL | 0.5588 mL | 1.3971 mL | |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4471 mL | 1.1176 mL | |
| 60 mM | 0.0373 mL | 0.1863 mL | 0.3725 mL | 0.9314 mL | |
| 80 mM | 0.0279 mL | 0.1397 mL | 0.2794 mL | 0.6985 mL | |
| 100 mM | 0.0224 mL | 0.1118 mL | 0.2235 mL | 0.5588 mL |
M351-0056 関連分類
HY-169853 関連分類
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Keywords
- M351-0056
- 1189495-81-5
- VISTA
- JAK
- STAT
- IFNAR
- NF-κB
- Interleukin Related
- TNF Receptor
- V-domain Ig suppressor of T cell activation (VISTA)
- Janus kinase
- Interferon-α/β receptor
- Interferon-alpha/beta receptor
- Nuclear factor-κB
- Nuclear factor-kappaB
- IL
- Tumor Necrosis Factor Receptor
- TNFR
- JAK2-STAT2 pathway
- peripheral blood mononuclear cell
- CD4+ T cell
- psoriasis-like skin inflammation
- T-cell
- Foxp3+ regulatory T cells
- IFN-I pathway
- noncanonical NF-κB pathway
- Jurkat E6.1 cells
- Inhibitor
- inhibitor
- inhibit