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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.48%
- No. CAS: 1189495-81-5
- Fòrmula: C15H12BrFN2O2S3
- Peso molecular:447.37
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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JAK2 |
STAT2 |
IL-17A |
IL-2 |
IL-1β |
M351-0056 (serial dilution; 30 min) binds to purified hVISTA-ECD protein with a KD value of 12.60 μM[1].
M351-0056 (5-50 μM; 48 h) enhances VISTA-mediated inhibition of IFN-γ, IL-17A, TNF-α and IL-2 secretion in activated peripheral blood mononuclear cells (PBMCs), with the strongest effect observed at 50 μM after 48 h[1].
M351-0056 (10 μM) enhances VISTA-mediated conversion of peripheral blood mononuclear cells (PBMCs) into CD4+Foxp3+ regulatory T cells[1].
M351-0056 (25-50 μM; 48 h) enhances the inhibitory effect of VISTA on IL-2 secretion in Jurkat E6.1 cells stimulated with PHA (HY-N7038)/PMA (HY-18739), with significant effects observed after treatment at concentrations of 25 μM and 50 μM for 48 h[1].
M351-0056 regulates the function of VISTA in peripheral blood mononuclear cells (PBMC) by reducing the mRNA expression of key genes in the JAK2-STAT2 signaling pathway[1].
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.
M351-0056 (50 mg/kg/day; i.g.; daily; 28 days) attenuates systemic lupus erythematosus in cGVHD mice via reducing renal dysfunction, autoantibody levels, renal pathology, and activation of IFN-I and noncanonical NF-κB pathways[2].
M351-0056 (50 mg/kg/day; i.g.; daily; 42 days) alleviates spontaneous systemic lupus erythematosus in MRL/lpr mice by reducing lymphoid organ enlargement, renal dysfunction, autoantibody levels, renal pathology, immune cell activation, and activation of IFN-I and noncanonical NF-κB pathways[2].
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.
Chemical Information
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No. CAS 1189495-81-5
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Appearance Solid
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Peso molecular 447.37
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
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