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PCNA-I1 DNA/RNA Synthesis activator

Name: PCNA-I1
Brand: Selleck Chemicals
SKU: S4476
Availability: InStock
Rating: 5 (1 reviews)

Catalog No.S4476 Purity:99.97%

PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). This compound selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. It inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. This chemical induces DNA damage and apoptosis in both LNCaP and PC-3 cells. It also induces autophagy in PC-3 cells.

Chemical Structure

Molecular Weight: 310.37

Purity & Quality Control

Batch: Purity: 99.97%

99.97

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Signaling Pathway

DNA/RNA Synthesis Signaling Pathway

Mechanism of Action

Targets

PCNA trimers ^[1]
(Cell-free assay)

0.2 to 0.4 μM(Kd)

In vitro
In vitro	PCNA-I1 prevents the transportation of the Proliferating Cell Nuclear Antigen (PCNA) to the cytoplasm by stabilizing its trimer form in the nucleus, thus inhibits SARS-CoV-2 replication.^[3]
Cell Research	Cell lines	Vero E6 cells
	Concentrations	0.1, 1, 10 and 100 µM
	Incubation Time	96 h
	Method	Lung tissue sections A plaque assay was performed. Briefly, after seeding, Vero E6 (8 × 10⁵ cells per well, 6-well plates) were incubated overnight and infected with 200 PFU per well. PCNA-I1 or Verdinexor were added at final concentrations of 0.5 µM or 0.1 µM and 0.1 µM or 1 µM, in overlays composed of DMEM supplemented with 10% FBS plus carboxymethylcellulose sodium salt 2%, immediately post-viral adsorption. A MTT cell proliferation assay was done to verify the toxicity of the drugs. After four days, cells were fixed with formaldehyde and stained with crystal violet to count plaques.

References

https://pubmed.ncbi.nlm.nih.gov/22399488/
https://pubmed.ncbi.nlm.nih.gov/25253786/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9168989/

Chemical Information

Molecular Weight	310.37	Formula	C₁₇H₁₄N₂O₂S
CAS No.	444930-42-1	SDF	--
Synonyms	N/A
Smiles	CC1=C(SC=C1)C(=O)N\N=C\C2=C(O)C3=CC=CC=C3C=C2

Storage and Stability

Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 62 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
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	1%DMSO 1 40%PEG300 2 5%TWEEN80 3 54%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.22mM)	Taking the 1 mL working solution as an example, add 10 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 540 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.750mg/ml (2.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.180mg/ml (0.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.6 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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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