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PRT4165 E3 Ligase inhibitor

Name: PRT4165
Brand: Selleck Chemicals
SKU: S5315
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S5315

PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.

Chemical Structure

Molecular Weight: 235.24

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Quality Control

Batch: Purity: 98.80%

98.80

Related Targets	Proteasome E1 Activating DUB p97 SUMO E2 conjugating
Other E3 Ligase Inhibitors	Skp2 inhibitor C1 (SKPin C1) Iberdomide (CC-220) Avadomide (CC-122) Apcin SZL P1-41 Mezigdomide (CC-92480) Homo-PROTAC cereblon degrader 1 MRT-2359 SMER3 SMIP004

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (46.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.200mg/ml (5.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	235.24	Formula	C₁₅H₉NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	31083-55-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC600157			Smiles	C1=CC=C2C(=C1)C(=O)C(=CC3=CN=CC=C3)C2=O

Mechanism of Action

Targets/IC₅₀/Ki	Bmi1/Ring1A 3.9 μM BMI-1 (Cell-free assay) 3.9 μM
In vitro	PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. It inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs. This compound inhibits both RNF2 and RING 1A, which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes, but not RNF8 nor RNF168. U2OS cells treated with increasing concentrations of this chemical show increasing numbers of cells in G2/M.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19956605/ [2] https://pubmed.ncbi.nlm.nih.gov/23902761/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4867636/#b31

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Handling Instructions

Tel: +1-832-582-8158 Ext:3

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