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Cat. No.: HY-184243

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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.

CAS No.: 3099924-90-7
Formula: C₂₁H₁₈ClF₂N₃O₄
Molecular Weight:449.84

Storage:

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

ISR/ROS-activator-1 Chemical Structure

CAS No.: 3099924-90-7

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Fluorescent Dye

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

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

Biological Activity

Description

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.

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	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	F	V_z
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.

Chemical Information

CAS No. 3099924-90-7
Molecular Weight 449.84
Formula C₂₁H₁₈ClF₂N₃O₄
SMILES

O=C1C(Cl)=C(C(C2=C1C(O)=CC=C2O)=O)NC3=CC(F)=C(N4CCN(CC4)C)C(F)=C3
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

Handling Instructions (2659 KB)

References

[1]. Zhang B, et al. Design, Synthesis, and Antitumor Evaluation of Novel Shikonin Derivatives: Discovery of 3k as a Dual Activator of the Integrated Stress Response and ROS in Gastric Cancer. J Med Chem. 2026 Jun 11;69(11):13121-13140. [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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100 mg

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