1. GPCR/G Protein
    Neuronal Signaling
    Apoptosis
  2. 5-HT Receptor
    Apoptosis
  3. PU02

PU02 

目录号: HY-103118 纯度: >99.0%
产品使用指南

PU02 是 6-MP (HY-13677) 的一个衍生物,是 5-HT3 受体的负变构调节剂,其在 HEK293 细胞测得的转染 5-HT3A 和 5-HT3AB 受体后的 IC50 值分别为 0.36 和 0.73 μM。

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PU02 Chemical Structure

PU02 Chemical Structure

CAS No. : 313984-77-9

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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].

IC50 & Target[1]

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.
Molecular Weight

292.36

Formula

C₁₆H₁₂N₄S

CAS No.

313984-77-9

SMILES

C12=NC=NC(SCC3=C4C=CC=CC4=CC=C3)=C1N=CN2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

References

Purity: >99.0%

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Keywords:

PU02PU 02PU-025-HT ReceptorApoptosisSerotonin Receptor5-hydroxytryptamine Receptorcyclin B1cyclinD1CDK4HepG2Inhibitorinhibitorinhibit

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PU02
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HY-103118
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