VU0359595是一种选择性磷脂酶 D1 (PLD1) 抑制剂,IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。
产品描述
VU0359595 is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.
体外活性
VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells. VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2]. VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3]. VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4]. VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].
Cas No.
1246303-14-9
分子式
C25H29BrN4O2
分子量
497.43
别名
ML-270;VU0359595-1
储存和溶解度
DMSO:5 mg/mL (10.1 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years