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CAS No.: 1130067-06-9

VU0155069 Catalog No. CSN23873

Synonyms: CAY10593

VU-0155069 is a selective phospholipase D1 (PLD1) inhibitor with IC50 values of 46 and 933 nM for PLD1 and PLD2 respectively.

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400-920-2911

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实验方案

技术信息

生物活性

描述Phospholipase D (PLD) is an essential enzyme responsible for the production of the lipid second messenger phosphatidic acid. This class of enzymes may play a role in numerous cellular pathways, including signal transduction, membrane trafficking, and the regulation of mitosis. PLD1 and PLD2 are the two reported mammalian isoforms of PLD. PLD1 has low basal activity that is highly regulated by protein kinase C (PKC), Arf and Rho GTPases, whereas PLD2 has high basal activity and mediates a number of unique protein interactions. VU-0155069 (also termed CAY10593) is a PLD1 selective inhibitor. Based on an enzyme activity assay, the inhibitory IC₅₀s of VU-0155069 against PLD1 and PLD2 are 46 nM and 933 nM, respectively. Alternatively, in cellular systems, the inhibitory IC₅₀s of VU-0155069 against PLD1 and PLD2 are 11 nM and 1800 nM, respectively. In transwell invasion assays performed in MDA-MB-231, 4T1 or PMT cells, three well characterized highly metastatic breast cancer cell lines, VU-0155069 was tested at the concentration of 0.2 μM or 20 μM. The results indicated that both concentrations of VU-0155069 significantly inhibited migration of the three cell lines^[3]. According to another report in the setting of isolated rheumatoid arthritis synovial fibroblast (RASF) cells cultured in vitro, 10 μM VU-0155069 inhibited IL-6 mRNA level by ~25% in the stimulation of IL-17 and TNFα and also obviously suppressed IL-6 secretion when TNFα was applied as a single stimulus^[4].
动物研究
剂量
Mice: 2.7 mg/kg^[1] (i.p.); 10 mg/kg^[2] (s.c.)

给药途径
i.p., s.c.
参考文献

动物研究
剂量	Mice: 2.7 mg/kg^[1] (i.p.); 10 mg/kg^[2] (s.c.)
给药途径	i.p., s.c.

[1] Lu WJ, Chung CL, et al. An Antithrombotic Strategy by Targeting Phospholipase D in Human Platelets. J Clin Med. 2018 Nov 14;7(11). pii: E440.
[2] Lee SK, Kim YS, et al. VU0155069 inhibits inflammasome activation independent of phospholipase D1 activity. Sci Rep. 2019 Oct 4;9(1):14349.
[3] Scott SA, Selvy PE, Buck JR, Cho HP, Criswell TL, Thomas AL, Armstrong MD, Arteaga CL, Lindsley CW, Brown HA. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17. doi: 10.1038/nchembio.140. Epub 2009 Jan 11. PMID: 19136975; PMCID: PMC3798018.
[4] Friday SC, Fox DA. Phospholipase D enzymes facilitate IL-17- and TNFα-induced expression of proinflammatory genes in rheumatoid arthritis synovial fibroblasts (RASF). Immunol Lett. 2016 Jun;174:9-18. doi: 10.1016/j.imlet.2016.04.001. Epub 2016 Apr 4. PMID: 27058440.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1600 mL
- 10.7998 mL
- 21.5997 mL
- 5 mM
- 0.4320 mL
- 2.1600 mL
- 4.3199 mL
- 10 mM
- 0.2160 mL
- 1.0800 mL
- 2.1600 mL

技术信息

CAS号

1130067-06-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27ClN4O2

运输

蓝冰

分子量

462.97

别名

CAY10593

溶解度

DMSO	30.0 mg/mL (64.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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