MedChemExpress LLC (MCE)

MedChemExpress - Model BML-280 - 1158347-73-9

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

MCE China：BML-280

Brand：MedChemExpress (MCE)

Cat. No.HY-114095

CAS：1158347-73-9

Synonyms：VU0285655-1

Purity：99.64%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

IC50 & Target：PLD2 PLD1 IL-1β IL-8

References：

[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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。