SET2

Modify Date: 2023-01-29 09:36:17

SET2 Structure
SET2 structure
Common Name SET2
CAS Number 2313525-20-9 Molecular Weight 402.44
Density N/A Boiling Point N/A
Molecular Formula C17H21F3N4O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SET2


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].

 Names

Name SET 2
Synonym More Synonyms

 SET2 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
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

 Synonyms

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