SET2

Names

[ Name ]:
SET2

[Synonym ]:
N-(2-Furanylmethyl)-3-[[4-(methylpropylamino)-6-(trifluoromethyl)-2-pyrimidinyl]thio]propanamide

Biological Activity

[Description]:

SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Cancer

[Target]

TRPV2:0.46 μM (IC50)

[In Vitro]

SET2 (20 μM；24 小时) 消除表达 TRPV2 的 PC-3M 细胞的迁移[1]。 SET2 (20 μM；24 小时) 抑制瞬时共转染 TRPV2 和 LPAR1 的 HEK293T 细胞中的 2-APB 诱发电流[1]。 SET2 (20 μM；24 小时) 抑制 LPA (0.1 μM；3 分钟) 诱导的细胞质钙增加和 LPA 诱导的 PC-3M 细胞迁移[1]。 Cell Migration Assay [1] Cell Line: PC-3M prostate cancer cells Concentration: 0, 5 μM, 10 μM, and 20 μM Incubation Time: 24 hr and 48 hr Result: Inhibited cell migration of PC-3M cells, without inhibiting cell viability at 48 hours.

[References]

[1]. Chai H, et al. Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. J Med Chem. 2019 Feb 14;62(3):1373-1384.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₂₁F₃N₄O₂S

[ Molecular Weight ]:
402.44

SET2

Names

Biological Activity

Chemical & Physical Properties

Related Compounds