2. Others NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Drug Derivative Reactive Oxygen Species (ROS) Apoptosis Ferroptosis
  4. ISR/ROS-activator-1

ISR/ROS-activator-1 is a naphthoquinone compound derived from Shikonin (HY-N0822), and also dual activator of the ISR/ROS pathway. ISR/ROS-activator-1 induces Apoptosis and Ferroptosis. ISR/ROS-activator-1 selectively inhibits gastric cancer. ISR/ROS-activator-1 is applicable to gastric cancer-related research.

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

ISR/ROS-activator-1

ISR/ROS-activator-1 Chemical Structure

CAS No. : 3099924-90-7

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ISR/ROS-activator-1 Related Antibodies

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Description

ISR/ROS-activator-1 is a naphthoquinone compound derived from Shikonin (HY-N0822), and also dual activator of the ISR/ROS pathway. ISR/ROS-activator-1 induces Apoptosis and Ferroptosis. ISR/ROS-activator-1 selectively inhibits gastric cancer. ISR/ROS-activator-1 is applicable to gastric cancer-related research[1].

In Vitro

ISR/ROS-activator-1 (Compound 3K) (72 h) selectively inhibits the viability of gastric cancer cells AGS, MGC-803, MKN-1 and MKN-45, with IC50 values ranging from 30.6 to 181.8 nM; it exhibits low toxicity to non-cancerous gastric epithelial cells GES-1, with an IC50 of 629 nM[1].
ISR/ROS-activator-1 (0.63-5 μM; 12 h) inhibits the long-term clonogenic survival of AGS and MKN-1 gastric cancer cells in a dose-dependent manner within the concentration range of 0.63 to 5 μM, while exerts weak effects on GES-1 non-cancerous gastric epithelial cells[1].
ISR/ROS-activator-1 (2.5 μM; 2 h) enhances the antiproliferative activity of 5-fluorouracil, Cisplatin and Irinotecan against AGS gastric cancer cells[1].
ISR/ROS-activator-1 (1.25 μM; 6 h) induces changes in protein expression in AGS gastric cancer cells, thereby activating the endoplasmic reticulum stress pathway, reducing antioxidant/mitochondrial function, and promoting ROS accumulation[1].
ISR/ROS-activator-1 (2.5 μM; 0.5-24 h) activates the integrated stress response (ISR) in AGS gastric cancer cells via rapid phosphorylation of eIF2α, and subsequently induces apoptosis marked by cleaved PARP and cleaved caspase-3 in a time-dependent manner[1].

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

ISR/ROS-activator-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: AGS, MGC-803, MKN-1, MKN-45, GES-1
Concentration: A series of concentrations
Incubation Time: 72 h
Result: Potently inhibited viability of all tested gastric cancer cell lines with IC50 values of 30.6 nM (AGS), 86.5 nM (MGC-803), 140.8 nM (MKN-1), and 181.8 nM (MKN-45).
Exhibited lower toxicity toward noncancerous GES-1 cells, with an IC50 of 629 nM.
Showed up to 10-fold greater potency relative to the parent compound shikonin.

Western Blot Analysis[1]

Cell Line: AGS
Concentration: 2.5 μM
Incubation Time: 0.5 h, 1 h, 2 h, 6 h, 12 h, 24 h
Result: Triggered a rapid increase in phosphorylated eIF2α (p-eIF2α) within 0.5-2 h, followed by a decline below basal levels at 6 h.
The decrease in p-eIF2α was accompanied by a gradual increase in cleaved PARP and cleaved caspase-3, markers of apoptosis.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ F Vz
Rat[1] 2 mg/kg i.v. 1.16 h / 115.78 ng/mL 88.99 ng·h/mL 91.64 ng·h/mL 1.11 h 1.34 h / 38058.76 mL/kg
Rat[1] 10 mg/kg p.o. 2.29 h 0.25 h 44.91 ng/mL 59.89 ng·h/mL 66.70 ng·h/mL 2.12 h 3.12 h 13.46 % /
Rat[1] 5 mg/kg i.p. 3.60 h 0.08 h 74.32 ng/mL 35.92 ng·h/mL 41.15 ng·h/mL 1.37 h 2.70 h 16.14 % /
In Vivo

ISR/ROS-activator-1 (1.0 mg/kg; i.p.; twice weekly; for 14 consecutive days) exhibits potent in vivo anti-tumor activity in the MKN-45 gastric cancer xenograft model[1].

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

Animal Model: Nude mice (n=6)[1]
Dosage: 1.0 mg/kg
Administration: i.p.; twice weekly; 14 days
Result: Achieved 77.4% tumor growth inhibition, which was greater than the 60.6% inhibition observed with cisplatin under tested conditions.
Significantly reduced tumor weight compared to the control group.
Molecular Weight

449.84

Formula

C21H18ClF2N3O4
CAS No.
SMILES

O=C1C(Cl)=C(C(C2=C1C(O)=CC=C2O)=O)NC3=CC(F)=C(N4CCN(CC4)C)C(F)=C3
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Purity & Documentation
References
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ISR/ROS-activator-1 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

ISR/ROS-activator-13099924-90-7Drug DerivativeReactive Oxygen Species (ROS)ApoptosisFerroptosisDrug derivativeapoptosisferroptosisgastric cancerAGSMKN-45gastric cancer cellsMGC-803gastric cancer xenograft modelsnormal gastric epithelial cellsMKN-1Inhibitorinhibitorinhibit

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