Art. -Nr.: HY-157435

PELI1-IN-1

Name: PELI1-IN-1
Brand: MedChemExpress
SKU: HY-157435
Price: 530.00 USD
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PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (K_d = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.

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Reinheit: 98.02%
CAS. Nr.: 3034889-94-3
Formel: C₂₀H₁₆O₄
Molecular Weight:320.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PELI1-IN-1 Chemical Structure

CAS. Nr.: 3034889-94-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	29.1 μM Compound: A4	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
MDA-MB-231	IC₅₀	31.2 μM Compound: A4	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]

In Vitro

PELI1-IN-1 (0-20 μM, 24-72 h) exhibits strong anti-migration activities without compromising the cell viability in MDA-MB-231^[1].
PELI1-IN-1 (0-20 μM, 24 h) significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression in MDA-MB-231 cells^[1].
PELI1-IN-1 (48 h) markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of EMT effectors SNAIL/SLUG in MDA-MB-231 cells^[1].

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

Cell Migration Assay ^[1]

Cell Line:

MDA-MB-231
Concentration:

0, 10 μM, 20 μM
Incubation Time:

24 h, 48 h
Result:

Inhibited the migration of MDA-MB-231 cells, with a relative migration rate of only 29.8 %.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231
Concentration:

0, 10 μM, 20 μM
Incubation Time:

0 h, 24 h, 48 h,72 h
Result:

Did not affect TNBC cell proliferation at concentrations that effectively inhibited cell migration.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

0, 10 μM, 20 μM
Incubation Time:

24 h
Result:

Significantly reduced the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression.

In Vivo

PELI1-IN-1 (50 mg/kg, oral gavage, once daily for 4 weeks) suppresses MDA-MB231 cell metastasis and shows no behavioral abnormality and significant body weight loss in NXG mice, suggesting the low toxicity of PELI1-IN-1^[1].

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

Animal Model:

MDA-MB-231 cells stably expressed luciferase were injected into NXG mice (Cavens) via tail^[1].
Dosage:

50 mg/kg
Administration:

Oral gavage, once daily for 4 weeks
Result:

Suppressed MDA-MB231 cell metastasis as evidenced by lower luciferase intensity in the lung.
Showed no behavioral abnormality (lethargy, clonic convulsion, anorexia, or ruffled fur) and significant body weight loss.

Chemical Information

CAS. Nr. 3034889-94-3
Appearance Solid
Molecular Weight 320.34
Formel C₂₀H₁₆O₄
Color Off-white to light yellow
SMILES

OC1=CC(O)=CC(/C=C/C2=C(C=CC(C3=CC=CC(O)=C3)=C2)O)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (312.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1217 mL

15.6084 mL

31.2168 mL

5 mM

0.6243 mL

3.1217 mL

6.2434 mL

10 mM

0.3122 mL

1.5608 mL

3.1217 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Resveratrol-derived inhibitors of the E3 ubiquitin ligase PELI1 inhibit the metastasis of triple-negative breast cancer. Eur J Med Chem. 2023 Dec 20:265:116060. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1217 mL	15.6084 mL	31.2168 mL	78.0421 mL
	5 mM	0.6243 mL	3.1217 mL	6.2434 mL	15.6084 mL
	10 mM	0.3122 mL	1.5608 mL	3.1217 mL	7.8042 mL
	15 mM	0.2081 mL	1.0406 mL	2.0811 mL	5.2028 mL
	20 mM	0.1561 mL	0.7804 mL	1.5608 mL	3.9021 mL
	25 mM	0.1249 mL	0.6243 mL	1.2487 mL	3.1217 mL
	30 mM	0.1041 mL	0.5203 mL	1.0406 mL	2.6014 mL
	40 mM	0.0780 mL	0.3902 mL	0.7804 mL	1.9511 mL
	50 mM	0.0624 mL	0.3122 mL	0.6243 mL	1.5608 mL
	60 mM	0.0520 mL	0.2601 mL	0.5203 mL	1.3007 mL
	80 mM	0.0390 mL	0.1951 mL	0.3902 mL	0.9755 mL
	100 mM	0.0312 mL	0.1561 mL	0.3122 mL	0.7804 mL

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PELI1-IN-1

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen