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.
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: 99.64%
- CAS 番号: 1158347-73-9
- 分子式: C25H27N5O2
- 分子量:429.51
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保管条件:Powder -20°C, 3 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
- 純度とドキュメンテーション
- 参考文献
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Phospholipase アイソフォーム固有の製品をすべて表示
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生物活性
|
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.
化学情報
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CAS 番号 1158347-73-9
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性状 Solid
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分子量 429.51
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分子式 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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別名
VU0285655-1
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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取扱説明書 (2659 KB)
参考文献
[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 |
BML-280 関連分類
HY-114095 関連分類
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