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Cat. No.: HY-180281

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PLAGL2-IN-1

PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a K_d of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC.

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

CAS No.: 3099026-16-8
Formula: C₃₀H₃₅Cl₂N₅O₄S
Molecular Weight:632.60

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

PLAGL2-IN-1 Chemical Structure

CAS No.: 3099026-16-8

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PLAGL2

2.23 μM (Kd)

All PI3K Isoforms :

All Akt Isoforms :

In Vitro

PLAGL2-IN-1 (compound C8) (72 h) demonstrates broad-spectrum antiproliferative activity in a panel of cancer cells, with IC₅₀s of 0.96 (A549), 1.35 (NCI-H1650), 1.03 (NCI-H460), 3.31 (MGC803), 3.28 (HGC27), 7.63 (SW620), 0.92 (HT29), 1.64 (MDA-MB-231), 2.21 (HCC1937), 1.43 (U87-MG), 24.96 (LN229), 8.83 (U937), 5.67 (K562), 5.33 (MEG01), 19.54 (Jurkat), 4.14 (PC-3), and 16.19 μM (SKOV3), respectively^[1].
PLAGL2-IN-1 (0-1 μM, 14 days) inhibits colony formation of MHCC-97H and HCCLM3 cells in a concentration-dependent manner^[1].
PLAGL2-IN-1 (10 μM, 48 h) induces apoptosis in MHCC-97H and HCCLM3 cells^[1].
PLAGL2-IN-1 (5 μM, 24 h) induces G0/G1 phase arrest in MHCC-97H cells^[1].
PLAGL2-IN-1 (0-10 μM, 48 h) inhibits cell migration and invasion in HCCLM3 and MHCC-97H cells in a dose-dependent manner, and demonstrates significant inhibition of cell division in HCCLM3 HCC cells^[1].
PLAGL2-IN-1 (5-10 μM, 24-48 h) disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation in HCCLM3 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MHCC-97H and HCCLM3
Concentration:

0, 0.01, 0.1, 1 μM
Incubation Time:

14 days
Result:

Resulted in a marked reduction incolony formation.
Showed concentration-dependent inhibition in both cells.

Apoptosis Analysis^[1]

Cell Line:

MHCC-97H and HCCLM3
Concentration:

10 μM
Incubation Time:

48 h
Result:

Induced late-stage apoptosis in both cells.
Exhibited stronger pro-apoptotic effects than the 5μM 5-FU (HY-90006) positive control.

Cell Cycle Analysis^[1]

Cell Line:

MHCC-97H and HCCLM3
Concentration:

5 μM
Incubation Time:

24 h
Result:

Induced G0/G1 phase arrest in MHCC-97H cells.
Did not induce cell cycle arrest in HCCLM3 cells.

Cell Migration Assay ^[1]

Cell Line:

MHCC-97H and HCCLM3
Concentration:

0, 5, 10 μM
Incubation Time:

48 h
Result:

Showed a dose-dependent inhibition of cell wound healing in HCCLM3 and MHCC-97H cells.
Inhibited cell migration in HCCLM3 and MHCC-97H cells.

Cell Invasion Assay^[1]

Cell Line:

MHCC-97H and HCCLM3
Concentration:

0, 5, 10 μM
Incubation Time:

48 h
Result:

Inhibited cell invasion in HCCLM3 and MHCC-97H cells in a dose-dependent manner.

Immunofluorescence^[1]

Cell Line:

HCCLM3
Concentration:

5 μM
Incubation Time:

48 h
Result:

Reduced the protein expression levels Vimentin.
Increased E-cadherin expression.

Western Blot Analysis^[1]

Cell Line:

HCCLM3
Concentration:

5, 10 μM
Incubation Time:

48 h
Result:

Reduced theprotein expression levels of ZEB1, Vimentin, MMP2, and MMP9.
Increased E-cadherin expression.
Significantly inhibited PLAGL2-dependent AKT phosphorylation at both Thr308 and Ser473.

In Vivo

PLAGL2-IN-1 (compound C8) (15 mg/kg, i.p., daily for 19 days) significantly inhibits tumor growth in a HCCLM3 xenograft mouse model without observable toxicity^[1].

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

Animal Model:

Male BALB/C nude mice (6-8 weeks old) subcutaneously injected with HCCLM3 cells^[1]
Dosage:

15 mg/kg
Administration:

i.p., daily for 19 days
Result:

Effectively inhibited tumor growth, with a TGI of 63.27%.
Significantly reduced tumor weight and volume.
Showed no observable toxicity in major organs but induced noticeable tumornecrosis.
Reduced expression of Ki-67 and α-SMA in tumor tissues.
Demonstrated a stable body weight during administration.

Chemical Information

CAS No. 3099026-16-8
Molecular Weight 632.60
Formula C₃₀H₃₅Cl₂N₅O₄S
SMILES

O=S(C1=CC=C2C=CC=CC2=C1)(NC3=CC(C(N4CCN(C(C(Cl)Cl)=O)CC4)=O)=CC=C3N5CCN(C(C)C)CC5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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)

References

[1]. Ding Y, et al. Discovery of novel small molecule inhibitor targeting the tumor promoting effect of transcription factor PLAGL2. Eur J Med Chem. 2026;303:118471. [Content Brief]

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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.

Keywords

100 mg

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Biological Activity
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PLAGL2-IN-1

All PI3K Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PLAGL2-IN-1 Related Classifications

HY-180281 Related Classifications