PCNA-I1

Catalog No.S4476 Batch:S447602

Technical Data

Formula

C₁₇H₁₄N₂O₂S

Molecular Weight

310.37

CAS No.

444930-42-1

Solubility (25°C)*

In vitro

DMSO

15 mg/mL (48.32 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.18mg/ml	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.75mg/ml	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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

Targets

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

0.2 to 0.4 μM(Kd)

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]

Protocol (from reference)

Cell Assay:^{^[3]}	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.

Cell Assay:^{^[3]}

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.