2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme Cytochrome P450 Proteasome
  4. PELI1-IN-1

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 (Kd = 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.

For research use only. We do not sell to patients.

PELI1-IN-1

PELI1-IN-1 Chemical Structure

CAS No. : 3034889-94-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PELI1-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 (Kd = 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[1].

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.

PELI1-IN-1 Related Antibodies

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.
Molecular Weight

320.34

Formula

C20H16O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1217 mL 15.6084 mL 31.2168 mL
5 mM 0.6243 mL 3.1217 mL 6.2434 mL
View the Complete Stock Solution Preparation Table

* 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.

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  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PELI1-IN-13034889-94-3E1/E2/E3 EnzymeCytochrome P450ProteasomeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCYPsPELI1Triple-negative breast cancerTNBCEpithelial-mesenchymal transitionEMTSNAIL/SLUGInhibitorinhibitorinhibit

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