BMS-561392 formate
Based on 2 publication(s) in Google Scholar
BMS-561392 formate (DPC 333 formate) is a selective ADAM17(TACE) inhibitor. BMS-561392 formate inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 formate also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 formate promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 formate can be used in research related to spinal cord injury and inflammatory diseases.
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- Pureté : 99.13%
- CAS No.: 2922280-85-9
- Formule: C28H34N4O6
- Masse moléculaire:522.59
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BMS-561392 formate
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Activité biologique
Description
In Vitro
BMS-561392 formate (10 nM; 1-2.5 h) potently inhibits recombinant human TACE (ADAM17) enzymatic activity by ~80%[1].
BMS-561392 formate (10 μM; 1 h pre-incubation followed by 4 h LPS stimulation) effectively suppresses LPS-induced TNF-α secretion in RAW264.7 macrophage cells[1].
BMS-561392 formate (1-100 μM; 1 h pre-incubation followed by 4 h LPS stimulation) dose-dependently inhibits LPS-induced p-IκB expression, and thus NFκB pathway activation, in RAW264.7 macrophage cells[1].
BMS-561392 formate (1-100 μM; 1 h pre-incubation followed by 1 h LPS stimulation) inhibits LPS-induced p-NFκB expression in RAW264.7 macrophage cells[1].
BMS-561392 formate (0.3-2.7 mM; 48 h) reduces viability of undifferentiated HOG cells in a concentration-dependent manner, with the greatest reduction (89.5-93.5%) observed at 2.7 mM after 48 h incubation[2].
BMS-561392 formate (0.3-2.7 mM; 48 h) modulates viability of BV-2 microglial cells in a concentration-dependent manner after 48 h incubation, with a slight increase at 0.3 mM, 50% reduction at 1.3 mM, and 94% reduction at 2.7 mM[2].
BMS-561392 formate (1.3-2.7 mM) induces apoptosis in BV-2 microglial cells, as shown by increased activated caspase-3-positive cells[2].
BMS-561392 formate (2.7 mM; 3 h) increases membrane TNFR-1 expression in BV-2 microglial cells by >50% after 3 h incubation[2].
BMS-561392 formate (0.3-2.7 mM; 3 h) modulates phosphorylated p44 MAPK levels in BV-2 microglial cells in a concentration-dependent manner after 3 h incubation, increasing levels at 0.3 mM and eliminating detectable levels at 2.7 mM, with no effect on phosphorylated p42 MAPK[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 macrophage cells
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Concentration:10 μM (pre-incubation); 1 μg/mL (LPS stimulation)
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Incubation Time:1 h (pre-incubation); 4 h (LPS stimulation)
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Result:Reduced LPS-induced TNF-α levels to near-control levels.
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Cell Line:RAW264.7 macrophage cells
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Concentration:1, 10 and 100 μM (pre-incubation); 1 μg/mL (LPS stimulation)
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Incubation Time:1 h (pre-incubation); 4 h (LPS stimulation)
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Result:Induced a dose-dependent reduction in LPS-stimulated p-IκB levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (10-week-old)[2]
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Dosage:2.2 mM
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Administration:s.c.; daily; 15 days
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Result:Significantly reduced locomotor recovery as measured by BMS score.
Significantly increased lesion size.
Significantly increased astrogliosis in tissue caudal to the lesion site.
Significantly reduced Iba1 expression in tissue rostro-caudal to the lesion epicenter.
Significantly increased the number of apoptotic microglial/macrophage cells in tissue caudal to the lesion site.
Significantly increased pro-apoptotic Bax expression in spinal cord tissue.
Showed a non-significant decrease in anti-apoptotic Bcl-2 expression in spinal cord tissue.
Chemical Information
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CAS No. 2922280-85-9
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Appearance Solid
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Masse moléculaire 522.59
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Formule C28H34N4O6
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Color White to off-white
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SMILES
OC=O.N[C@]1(C2=CC=C(C=C2)OCC3=CC(C)=NC4=C3C=CC=C4)C(N(CC1)[C@H](CC(C)C)C(NO)=O)=O
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Synonyms
DPC 333 formate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Curr Issues Mol Biol
Mechanistic Insights into Vorinostat as a Repositioned Modulator of TACE-Mediated TNF-α Signaling via MAPK and NFκB Pathways. [Abstract]2025 Sep 4;47(9):720. PMID: 41020841 -
PLoS One
Discovery of novel TACE inhibitors using graph convolutional network, molecular docking, molecular dynamics simulation, and Biological evaluation. [Abstract]2024 Dec 27;19(12):e0315245. PMID: 39729480
Solvant et solubilité
In Vitro:
DMSO : ≥ 125 mg/mL (239.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (302 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Park J, et al. Mechanistic Insights into Vorinostat as a Repositioned Modulator of TACE-Mediated TNF-α Signaling via MAPK and NFκB Pathways. Curr Issues Mol Biol. 2025 Sep 4;47(9):720. [Content Brief]
[2]. Vidal PM, et al. ADAM17 is a survival factor for microglial cells in vitro and in vivo after spinal cord injury in mice. Cell Death Dis. 2013 Dec 12;4(12):e954. [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 (sealed storage, away from moisture). 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 | 1.9135 mL | 9.5677 mL | 19.1355 mL | 47.8386 mL |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.8271 mL | 9.5677 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9135 mL | 4.7839 mL | |
| 15 mM | 0.1276 mL | 0.6378 mL | 1.2757 mL | 3.1892 mL | |
| 20 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3919 mL | |
| 25 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9135 mL | |
| 30 mM | 0.0638 mL | 0.3189 mL | 0.6378 mL | 1.5946 mL | |
| 40 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1960 mL | |
| 50 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 60 mM | 0.0319 mL | 0.1595 mL | 0.3189 mL | 0.7973 mL | |
| 80 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5980 mL | |
| 100 mM | 0.0191 mL | 0.0957 mL | 0.1914 mL | 0.4784 mL |
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