Cat. No.: HY-149717

Antitumor agent-122

Antitumor agent-122 is a potent multi-target antitumor agent that exerts its effects through the induction of ferroptosis, autophagy, apoptosis, and cell cycle arrest. In the ferroptosis pathway, Antitumor agent-122 inhibits GPX4 expression and upregulates FACL4 expression, increasing intracellular lipid peroxidation and ferrous ion levels. In the autophagy pathway, Antitumor agent-122 induces autophagy by inhibiting the AKT/mTOR signaling pathway. In the apoptosis and cell cycle pathways, Antitumor agent-122 arrests cells at the G1/S phase and subsequently promots mitochondrial pathway-mediated apoptosis. Antitumor agent-122 can be used in the research of solid tumors including gastric, liver, ovarian, and bladder cancers.

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

CAS No.: 2378641-43-9
Formula: C₂₈H₃₀N₄O₂S₂
Molecular Weight:518.69

Storage:

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

Data Sheet (277 KB)

Antitumor agent-122 Chemical Structure

CAS No.: 2378641-43-9

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

GPX4

ACSL4

All Glutathione Peroxidase Isoforms :

GPX1
GPX4

All Akt Isoforms :

All mTOR Isoforms :

All ERK Isoforms :

All ACSL Family Isoforms :

ACSL4
ACSL5

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	3.6 μM Compound: 5j	Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay	[PMID: 37972528]
HK-2	IC₅₀	14.92 μM Compound: 5j	Antiproliferative activity against human HK-2 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HK-2 cells incubated for 48 hrs by MTT assay	[PMID: 37972528]
HUVEC	IC₅₀	16.74 μM Compound: 5j	Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay	[PMID: 37972528]
MGC-803	IC₅₀	5.23 μM Compound: 5j	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by MTT assay	[PMID: 37972528]
SK-OV-3	IC₅₀	1.43 μM Compound: 5j	Antiproliferative activity against human SK-OV-3 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells incubated for 48 hrs by MTT assay	[PMID: 37972528]
T-24	IC₅₀	3.03 μM Compound: 5j	Antiproliferative activity against human T24 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human T24 cells incubated for 48 hrs by MTT assay	[PMID: 37972528]

In Vitro

Antitumor agent-122 (compound 5j) inhibits the proliferation of MGC-803, HepG-2, SKOV-3, and T24 cells, with IC₅₀ values of 5.23, 3.60, 1.43, and 3.03 μM, respectively^[1].
Antitumor agent-122 exhibits low cytotoxicity in HK2 and HUVEC cells, with IC₅₀ values of 14.92 and 16.74 μM, respectively^[1].
Antitumor agent-122 inhibits the proliferation of cisplatin-resistant A549/DDP cells^[1].
Antitumor agent-122 (5 μM; 24 h) induces ferroptosis in T24 cells by downregulating GPX4 expression, upregulating ACSL4 expression, and promoting the accumulation of lipid peroxides, ferrous ions, superoxide anions, and ROS^[1].
Antitumor agent-122 (5 μM; 24 h and 48 h) induces ferroptosis-like mitochondrial morphological changes and autophagosome formation in T24 cells^[1].
Antitumor agent-122 (2, 5, 8 μM; 24 h) induces autophagy in T24 cells by upregulating LC3B, downregulating P62, inhibiting AKT/mTOR-related signaling, and activating ERK signaling^[1].
Antitumor agent-122 (1–5 μM; 7 days) reduces colony formation in T24 cells^[1].
Antitumor agent-122 (1–10 μM; 0, 24, 48 h) inhibits T24 cell migration, and its anti-migratory effect is attenuated by the ERK inhibitor FR180204 (HY-12275)^[1].
Antitumor agent-122 (2, 5, 8 μM; 24 h) promotes mitochondrial pathway-mediated apoptosis in T24 cells by upregulating the expression of cleaved-caspase 3, cleaved-PARP, Bax, Bak, and Bad^[1].
Antitumor agent-122 (2, 5, and 8 μM; 24 h) upregulates p21 and downregulates MCM5 in T24 cells, inducing G1/S phase cell cycle arrest^[1].

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

Western Blot Analysis^[1]

Cell Line:

T24
Concentration:

5 μM
Incubation Time:

24 h
Result:

Markedly decreased intracellular GPX4 levels and increased FACL4 expression.

Western Blot Analysis^[1]

Cell Line:

T24
Concentration:

2, 5, 8 μM
Incubation Time:

24 h
Result:

Upregulated LC3B and decreased P62, confirming autophagy induction. Decreased phosphorylated AKT1, AKT1 and mTOR expression, and induced ERK1/2 phosphorylation in a dose-dependent manner.
Upregulated cleaved-caspase 3, cleaved-PARP, Bax, Bak and Bad.

Cell Proliferation Assay^[1]

Cell Line:

T24
Concentration:

1, 2, 3, 4, 5 μM
Incubation Time:

7 days
Result:

Reduced colony formation at different concentrations.

Cell Migration Assay ^[1]

Cell Line:

T24
Concentration:

1, 5, 7, 10 μM; FR180204 at 1, 2, 3 μM
Incubation Time:

0, 24, 48 h
Result:

Inhibited T24 cell migration in a time- and concentration-dependent manner. Co-incubation with ERK inhibitor FR180204 (HY-12275) reduced the antimigratory effect.

Cell Cycle Analysis^[1]

Cell Line:

T24
Concentration:

2, 5, 8 μM
Incubation Time:

24 h
Result:

Induced G1/S cell cycle arrest in a concentration-dependent manner. The result was consistent with omics analysis and indicated cell cycle blockade after treatment.
Upregulated p21 and downregulated MCM5.

In Vivo

Antitumor agent-122 (compound 5j) (5, 15 mg/kg; i.p.; once every two days; for 21 days) has antitumor activity in T24 xenograft nude mouse model^[1].
Antitumor agent-122 (5, 15 mg/kg; intraperitoneal injection; once every two days; for 21 days) has antitumor activity with limited toxicity in HepG-2 xenograft nude mouse model^[1].
Antitumor agent-122 (5, 15 mg/kg; i.p.; once every two days; for 21 days) exhibits antitumor activity in SKOV-3 xenograft nude mouse model^[1].

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

Animal Model:

T24 xenograft nude mouse model^[1]
Dosage:

5, 15 mg/kg
Administration:

Intraperitoneal injection (i.p.); once every two days; for 21 days
Result:

Suppressed T24 xenograft tumor growth. At 15 mg/kg, achieved a tumor inhibition ratio (TIR) of 56.3%, exceeding the effective antitumor threshold of 40%.
Showed lower antitumor activity in the low-dose group than in the high-dose group, indicating a dose-dependent effect.
Did not cause obvious severe body weight loss during treatment, suggesting acceptable tolerability.

Animal Model:

HepG-2 xenograft nude mouse model^[1]
Dosage:

5, 15 mg/kg
Administration:

Intraperitoneal injection (i.p.); once every two days; for 21 days
Result:

Suppressed HepG-2 xenograft tumor growth. At 15 mg/kg, achieved a TIR of 50.0%, indicating effective in vivo antitumor activity.
Showed lower antitumor activity in the low-dose group than in the high-dose group.
Reduced tumor volume and tumor weight compared with vehicle group.
Showed less tissue toxicity than amonafide in heart, liver, spleen and lung pathological sections.

Animal Model:

SKOV-3 xenograft nude mouse model^[1]
Dosage:

5, 15 mg/kg
Administration:

Intraperitoneal injection (i.p.); once every two days; for 21 days
Result:

Exhibited antitumor activity in SKOV-3 xenograft model.
Showed significantly less toxicity than amonafide in heart, liver, spleen and lung pathological sections, with the lowest comprehensive toxicity among all tested compounds, and was thus selected for further mechanistic investigation.

Chemical Information

CAS No. 2378641-43-9
Molecular Weight 518.69
Formula C₂₈H₃₀N₄O₂S₂
SMILES

S=C(N1CCN(C2=CC=C(C3=C4C=CC=C32)C(N(CCN(C)C)C4=O)=O)CC1)SCC5=CC=CC=C5
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 (277 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]. Liang SM et al. Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance. Eur J Med Chem. 2024 Jan 5;263:115937. [Content Brief]

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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.

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Antitumor agent-122

All Glutathione Peroxidase Isoforms

All Akt Isoforms

All mTOR Isoforms

All ERK Isoforms

All ACSL Family Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Antitumor agent-122 Related Classifications

HY-149717 Related Classifications