PU 02

Modify Date: 2024-01-09 18:10:08

PU 02 Structure
PU 02 structure
Common Name PU 02
CAS Number 313984-77-9 Molecular Weight 292.35800
Density N/A Boiling Point N/A
Molecular Formula C16H12N4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PU 02


PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively[1][2].

 Names

Name 6-[(1-Naphthylmethyl)sulfanyl]-7H-purine
Synonym More Synonyms

 PU 02 Biological Activity

Description PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively[1][2].
Related Catalog
Target

5-HT3A Receptor:0.36 μM (IC50)

5-HT 3 AB:0.73 μM (IC50)

In Vitro PU02 (NMMP) (0-200 μM) leads to a steady decrease in cell viability of HepG2 cells (IC50=48.585 μM). PU02 (NMMP) shows less toxicity on L02 cells than did 6-MP after 48 h of treatment[2]. PU02 (NMMP) at 6.25 or 25 μM exhibits inhibitory effects on the viability of the tested cell lines, including SMMC-7721, MDA-MB-231, RKO and HCT-8 cells[2]. PU02 (NMMP) induces cell cycle arrest at the G2/M phase. PU02 (NMMP) downregulats the expression of cyclin B1/D1 and CDK4 in a time-dependent manner in HepG2 cells,but the expression of cyclin E is not affected[2]. PU02 (NMMP)-treated cells exhibits a significant increase in caspase-3 cleavage, suggesting enhanced apoptotic activity[2]. Apoptosis Analysis[2] Cell Line: HepG2 cells. Concentration: 6.26, 12.5, 25, 50 μM. Incubation Time: 6, 12, 24, 36 h. Result: Induced mitochondria-dependent apoptosis.
References

[1]. Sarah M Trattnig, et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54.

[2]. Xiao-Guang Yang, et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2012 Nov 15;695(1-3):27-33.

 Chemical & Physical Properties

Molecular Formula C16H12N4S
Molecular Weight 292.35800
Exact Mass 292.07800
PSA 79.76000
LogP 3.79840

 Safety Information

Hazard Codes Xi

 Synonyms

MFCD23381174
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