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

PU02 

Cat. No.: HY-103118 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

PU02 Chemical Structure

PU02 Chemical Structure

CAS No. : 313984-77-9

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10 mg USD 85 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (855.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4204 mL 17.1022 mL 34.2044 mL
5 mM 0.6841 mL 3.4204 mL 6.8409 mL
10 mM 0.3420 mL 1.7102 mL 3.4204 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
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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