1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. PRT4165

PRT4165 (Synonyms: NSC600157)

Cat. No.: HY-19817 Purity: >98.0%
Handling Instructions

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.

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

PRT4165 Chemical Structure

PRT4165 Chemical Structure

CAS No. : 31083-55-3

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 260 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

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.

IC50 & Target

PRC1[1]

In Vitro

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation. In vitro E3 ubiquitin ligase activity assays reveal that PRT4165 inhibits both RNF2 and RING 1A, but not RNF8 nor RNF168. In the presence of PRT4165, H2A ubiquitylation could be completely inhibited regardless of whether RING1 or RNF2 contributes the E3 ubiquitin ligase activity. Treatment of cells for 60 min with 50 μM PRT4165 results in a dramatic reduction in total ubiquitylated histone H2A. It is also found that longer exposure of the cells with the PRT4165 (30 and 60 min) leads to increased levels of γ-H2AX in unirradiated cells. PRT4165 inhibits double-strand break (DSB) repair at the 8-h time point compare with mock treated cells. Cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M[1].

Molecular Weight

235.24

Formula

C₁₅H₉NO₂

CAS No.

31083-55-3

SMILES

O=C1/C(C(C2=C1C=CC=C2)=O)=C/C3=CC=CN=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (106.27 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2510 mL 21.2549 mL 42.5098 mL
5 mM 0.8502 mL 4.2510 mL 8.5020 mL
10 mM 0.4251 mL 2.1255 mL 4.2510 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: ≥ 2.5 mg/mL (10.63 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (10.63 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (10.63 mM); Precipitated solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Cells are treated with different concentrations of the PRT4165 60 min prior to irradiation (2 Gy). The cells are harvested 2 h after IR. The cells are washed with PBS twice and then fixed with 1% paraformaldehyde at 37°C for 10 min. After cooling on ice for 1 min, the cells are permeabilized with 90% methanol and stored at -20°C overnight. Fixed cells are washed with PBS twice and blocked with FACS incubation buffer (0.5% BSA in PBS) for 10 min. The cells are then stained with anti-phosphohistone H3 (serine 10) antibody at 1:500 dilution in FACS incubation buffer for 1 h at room temperature[1].

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

References
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PRT4165
Cat. No.:
HY-19817
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