[CAS NO. 31083-55-3]  PRT4165

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PRODUCTS SPECIFICATIONS [31083-55-3]

Catalog
HY-19817
Brand
MCE
CAS
31083-55-3

DESCRIPTION [31083-55-3]

Overview

MDLMFCD00435709
Molecular Weight235.24
Molecular FormulaC15H9NO2
SMILESO=C1/C(C(C2=C1C=CC=C2)=O)=C/C3=CC=CN=C3

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


Summary

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 can 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 G 2 /M [1] .

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


Appearance

Solid


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)

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

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


Synonyms

1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)-
1,3-Indandione, 2-(3-pyridylmethylene)-
2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
2-(3-Pyridylmethylene)-1,3-indandione
NSC 600157
PRT 4165
SML 1013
2-(Pyridin-3-ylmethylidene)indene-1,3-dione
2-[(Pyridin-3-yl)methylidene]-2,3-dihydro-1H-indene-1,3-dione
2-Pyridin-3-ylmethylene-indan-1,3-dione