2. Apoptosis Autophagy Metabolic Enzyme/Protease PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. Ferroptosis Autophagy Apoptosis Glutathione Peroxidase Akt mTOR ERK ACSL Family
  4. 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.

Antitumor agent-122

Antitumor agent-122 Chemical Structure

CAS No. : 2378641-43-9

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Antitumor agent-122 Related Antibodies

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GPX1 GPX4

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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ACSL4 ACSL5

  • Biological Activity

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Description

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[1].

IC50 & Target[1]

GPX4

 

ACSL4

 

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.

Antitumor agent-122 Related Antibodies

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.
Molecular Weight

518.69

Formula

C28H30N4O2S2
CAS No.
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
References
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Antitumor agent-122 Related Classifications

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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:

Antitumor agent-1222378641-43-9Antitumor agent122Antitumor agent 122FerroptosisAutophagyApoptosisGlutathione PeroxidaseAktmTORERKACSL FamilyPKBProtein kinase BMammalian target of RapamycinExtracellular signal regulated kinasesmulti-target antitumor drugHepG-2SKOV-3MGC -803T24A549/DDPT24 xenograftHepG-2 xenograftSKOV-3 xenograftgastric cancerhepatocellular carcinomaovarian cancerbladder cancerInhibitorinhibitorinhibit

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