BML-280
Based on 1 Customer Validation
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.64%
- No. CAS: 1158347-73-9
- Fòrmula: C25H27N5O2
- Peso molecular:429.51
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Almacenamiento:Powder -20°C, 3 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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Solvente y solubilidad
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Ver todos los productos específicos de isoformas Phospholipase
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Actividad biológica
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PLD2 |
PLD1 |
IL-1β |
IL-8 |
BML-280 shows an approximately 21-fold selectivity for PLD2[3].
BML-280 (0-0.1 µM) suppresses formyl-Met-Leu-Phe (fMLP)-stimulated PLD activity in a concentration dependent manner, with an IC50 of 0.04 ± 0.01 μM[3].
BML-280 (0-0.3 µM) inhibits O2- generation, and the inhibition reaches a plateau (about 20 % inhibition) at around 0.01 μM to 0.3 μM[3].
BML-280 (0-5 µM, 24 h) reduces proliferation in PLD1-deficient cells, but also in PLD2-deficient cells exposed to IGF-1 (Insulin-like growth factor 1)[1].
BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells[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, PLD1- and PLD2-deficient astrocytes
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Concentration:0, 50, 500, and 5000 nM
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Incubation Time:24 h
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Result:Had minor effects in wild-type and PLD2-deficient cells, but completely blocked PLD activity in PLD1-deficient cells. Caused a highly significant inhibition of glial proliferation when astrocytes were stimulated by FCS (fetal calf serum) or IGF-1, respectively. Showed non-specific effects because they inhibited cell proliferation even in PLD1/2 double knockouts at 5 µM.
Chemical Information
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No. CAS 1158347-73-9
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Appearance Solid
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Peso molecular 429.51
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Fòrmula C25H27N5O2
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Color White to off-white
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SMILES
O=C(C1=CC2=CC=CC=C2N=C1)NCCN(CC3)CCC3(N(C4=CC=CC=C4)CN5)C5=O
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Synonyms
VU0285655-1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 125 mg/mL (291.03 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)
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Burkhardt U, et al. Role of phospholipases D1 and 2 in astroglial proliferation: effects of specific inhibitors and genetic deletion. Eur J Pharmacol. 2015 Aug 15;761:398-404. [Content Brief]
[2]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019 Jul;184:243-257. [Content Brief]
[3]. Tsai YR, et al. Inhibition of formyl peptide-stimulated phospholipase D activation by Fal-002-2 via blockade of the Arf6, RhoA and protein kinase C signaling pathways in rat neutrophils. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):507-19. [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 | 2.3282 mL | 11.6412 mL | 23.2823 mL | 58.2059 mL |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6565 mL | 11.6412 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL | 5.8206 mL | |
| 15 mM | 0.1552 mL | 0.7761 mL | 1.5522 mL | 3.8804 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1641 mL | 2.9103 mL | |
| 25 mM | 0.0931 mL | 0.4656 mL | 0.9313 mL | 2.3282 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7761 mL | 1.9402 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5821 mL | 1.4551 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1641 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9701 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7276 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5821 mL |
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