MBA-m1
Based on 1 Customer Validation
MBA-m1 is a reversible non-covalent allosteric inhibitor of mMLKL2, with a Kd value of 6 μM for mMLKL2. MBA-m1 delays Necroptosis. MBA-m1 has no effect on the activities of RIPK1 or RIPK3. MBA-m1 alleviates skin injury, epidermal thickening and immune cell infiltration in dermatitis models, and reduces aortic diameter enlargement and structural changes in abdominal aortic aneurysm models. MBA-m1 can be used in research related to dermatitis and abdominal aortic aneurysm.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.20%
- No. CAS: 305866-70-0
- Fòrmula: C27H21ClN2O2
- Peso molecular:440.92
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
7.07 μM
Compound: GNF-Pf-2622
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
| SK-BR-3 | IC50 |
5 μM
Compound: 33
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Cytotoxicity against human SKBr3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKBr3 cells after 72 hrs by MTT assay
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[PMID: 18500794] |
MBA-m1 (10 μM) potently delays TSZ-induced necroptosis in wild-type mouse NIH-3T3 cells by inhibiting mMLKL activation and downstream cell death processes[1].
MBA-m1 directly binds to purified recombinant mouse mMLKL2 protein, and this conclusion is confirmed by isothermal titration calorimetry[1].
MBA-m1 (10 μM; 1 h pre-treatment) binds to mMLKL in wild-type mouse NIH-3T3 cells, which is confirmed by the increased thermal stability of mMLKL in cellular thermal shift assay[1].
MBA-m1 (12.5-200 μM) binds to recombinant mouse MLKL (mMLKL2) with a Kd value of 6 μM[2].
MBA-m1 (4-8 h post TSZ treatment; 1-10 μM) dose-dependently delays the necroptosis kinetics of NIH-3T3 cells[2].
MBA-m1 (5-10 μM; 0-24 h post-TS treatment) does not affect RIPK1-mediated extrinsic apoptosis in wild-type or MLKL-knockout NIH-3T3 cells, which supports its specificity for MLKL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type and MLKL knockout NIH-3T3 cells
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Concentration:5, 10 μM
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Incubation Time:0-24 h (post-TS treatment)
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Result:Had no discernible effect on the kinetics of RIPK1-mediated extrinsic apoptosis in either wild-type or MLKL knockout NIH-3T3 cells.
MBA-m1 (30 mg/kg; i.p.; every other day; 18 days) significantly attenuates abdominal aortic aneurysm progression in mice, reducing aortic dilation, structural damage, and immune cell infiltration[1].
MBA-m1 significantly reduces dermatitis severity and disease progression in a necroptosis-driven mouse dermatitis model[2].
MBA-m1 prevents aortic aneurysm development in a porcine pancreatic elastase-induced mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N mice (30-40 days old)[1]
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Dosage:30 mg/kg
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Administration:i.p.; every other day; 21 days
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Result:Significantly ameliorated dermatitis with patches of healthy and moderately inflamed dorsal skin.
Reduced epidermal thickness compared to vehicle controls.
Decreased CD45-positive cell infiltration in both healthy and inflamed tissue compared to vehicle controls.
Lowered dermatitis severity scores at study endpoint compared to vehicle controls.
Chemical Information
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No. CAS 305866-70-0
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Appearance Solid
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Peso molecular 440.92
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Fòrmula C27H21ClN2O2
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Color White to off-white
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SMILES
ClC1=CC(NC2=CC(C)=NC3=C2C=C(OC)C=C3)=CC=C1OC4=CC5=C(C=CC=C5)C=C4
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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
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MBA-m1 Related Classifications
HY-24504 Related Classifications
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