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PRT4165 (NSC-600157)

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PRT4165 (NSC-600157)
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Cat #: V0083 CAS #: 31083-55-3 Purity ≥ 99%

Description: PRT4165 (NSC600157) is a potent and selective inhibitor of the PRC1 (polycomb repressive complex 1)-mediated H2A ubiquitylation with potential anticancer activity.

References: Ismail IH, et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J Biol Chem. 2013 Sep 13;288(37):26944-54.

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Molecular Weight (MW)235.24
Molecular FormulaC15H9NO2
CAS No.31083-55-3
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 11 mg/mL (46.8 mM)rr
Water: 4 mg/mL (17.0 mM)rr
Ethanol: < 1 mg/mL
SMILES CodeO=C1/C(C(C2=C1C=CC=C2)=O)=CC3=CC=CN=C3
SynonymsPRT4165, PRT-4165, PRT 4165; NSC600157; NSC 600157; NSC-600157
ProtocolIn VitroPRT4165 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 G2/M
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM4.2510 mL21.2549 mL42.5098 mL85.0196 mL
5mM0.8502 mL4.2510 mL8.5020 mL17.0039 mL
10mM0.4251 mL2.1255 mL4.2510 mL8.5020 mL
20mM0.2125 mL1.0627 mL2.1255 mL4.2510 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.