For research use only. Not for therapeutic Use.
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[1][2].
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].
| Catalog Number | I012129 |
| CAS Number | 1158347-73-9 |
| Synonyms | N-[2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl]quinoline-3-carboxamide |
| Molecular Formula | C25H27N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H27N5O2/c31-23(20-16-19-6-4-5-9-22(19)27-17-20)26-12-15-29-13-10-25(11-14-29)24(32)28-18-30(25)21-7-2-1-3-8-21/h1-9,16-17H,10-15,18H2,(H,26,31)(H,28,32) |
| InChIKey | WJOCDBUFEUKYNI-UHFFFAOYSA-N |
| SMILES | C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCNC(=O)C4=CC5=CC=CC=C5N=C4 |
| Reference | [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. [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. [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. |
