2. Apoptosis Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Ferroptosis DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis Reactive Oxygen Species (ROS)
  4. HJ03

HJ03 is a blood-brain barrier-permeable, orally active DNA damage and ferroptosis inducer. HJ03 triggers ferroptosis by increasing intracellular ROS, Fe2+ accumulation and lipid peroxidation. HJ03 induces DNA adducts and interstrand crosslinks, blocks DNA replication and transcription, arrests cells at the G2/M phase and induces apoptosis. HJ03 can be used in the research of glioblastoma multiforme and colorectal cancer.

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

HJ03

HJ03 Chemical Structure

CAS No. : 3028123-48-7

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HJ03 Related Antibodies

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Description

HJ03 is a blood-brain barrier-permeable, orally active DNA damage and ferroptosis inducer. HJ03 triggers ferroptosis by increasing intracellular ROS, Fe2+ accumulation and lipid peroxidation. HJ03 induces DNA adducts and interstrand crosslinks, blocks DNA replication and transcription, arrests cells at the G2/M phase and induces apoptosis. HJ03 can be used in the research of glioblastoma multiforme and colorectal cancer[1].

In Vitro

HJ03 (24-72 h) potently inhibits the viability of U251, U87, T98G, HCT116, MSH6-deficient U251 and MSH6-deficient T98G cells, with IC50 values ranging from 0.8914 μM to 61.65 μM after incubation for 24, 48, and 72 h. Its activity is independent of MGMT and MSH6 status[1].
HJ03 (0.25-8 μM; 14 days) inhibits colony formation of U251, U87 and T98G cells in a dose-dependent manner[1].
HJ03 (4-16 μM; 72 h) inhibits the viability of U87 spheroids and induces cell death, with 16 μM causing nearly complete spheroid death[1].
HJ03 (1-5 μM; 48-72 h) induces G2/M phase arrest in U251 and U87 cells, and regulates cell cycle-related proteins (p21, p-CDK1, CDK1, cyclin B1) in U251, U87 and T98G cells[1].
HJ03 (1-40 μM; 48-72 h) induces apoptosis in U251, U87 and T98G cells in a dose-dependent manner via cleavage of caspase-3/7/9 and PARP[1].
HJ03 (1-80 μM; 48-72 h) induces ferroptosis in U251, U87 and T98G cells through mechanisms involving upregulation of ROS, Fe2+ and MDA levels, downregulation of SLC7A11, as well as upregulation of p53 or ATF3[1].
HJ03 (0.4-50 μM; 15-72 h) induces DNA damage in U251, U87 and T98G cells through activating the ATM-Chk2 DNA damage response pathway; it also induces dose-dependent DNA cross-linking and alkylation in purified linearized pBR322 DNA[1].

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

HJ03 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: U251, U87, T98G
Concentration: 0.25, 0.5 andn 1 μM (U251); 1, 2 and 4 μM (U87); 2, 4 and 8 μM (T98G)
Incubation Time: 14 days
Result: Reduced colony formation significantly in U251 cells treated with 0.25, 0.5, or 1 μM compared to control.
Almost completely inhibited U87 cell colony formation at concentrations >2 μM.
Induced comparable colony formation inhibition in T98G cells treated with 2 μM to that of 50 μM TMZ.

Cell Viability Assay[1]

Cell Line: U87
Concentration: 4, 8 and 16 μM
Incubation Time: 72 h
Result: Induced U87 spheroid shrinkage and cell death at 4 μM.
Caused almost complete spheroid death at 16 μM.

Cell Cycle Analysis[1]

Cell Line: U251, U87, T98G
Concentration: 1, 2 and 4 μM (U251); 5 μM (U87)
Incubation Time: 48 h, 72 h
Result: Arrested 21.8%, 33%, and 70.3% of U251 cells in G2/M phase after 48 h treatment with 1, 2, 4 μM, respectively.
Increased G2/M arrest in U251 cells to 24.1%, 50.5%, and 67.8% after 72 h treatment with 1, 2, 4 μM, respectively.
Increased U87 cell G2/M arrest by >35% after 48 and 72 h treatment with 5 μM.
Increased p21 and p-CDK1, and decreased CDK1 and cyclin B1 in U251, U87, and T98G cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: U251, U87, T98G
Concentration: 1, 2 and 4 μM (U251); 5, 10 and 20 μM (U87); 10, 20 and 40 μM (T98G)
Incubation Time: 48 h, 72 h
Result: Induced significant apoptosis in U251 cells after 48 h incubation with 1, 2, 4 μM.
Triggered significant apoptosis in U87 cells after 48 h incubation with 5, 10, 20 μM.
Induced significant apoptosis in T98G cells after 48 h incubation with 20, 40 μM.
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) T1/2 Tmax (Brain)
Mice[1] 66 mg/kg p.o. 649.5 nM 0.25 h 0.4 h 0.5 h
In Vivo

HJ03 (2-20 mg/kg; p.o.; 5 consecutive days per week; 4 weeks) significantly prolongs survival in mice bearing orthotopic glioblastoma tumors[1].
HJ03 (2-132 mg/kg; p.o.; daily; 7 days) at doses up to 66 mg/kg is well-tolerated by healthy mice, with no significant weight loss or hematological toxicity, while the 132 mg/kg dose induces mild hematological toxicity[1].

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

Animal Model: C57BL/6 (male, 8 weeks old, intracranial stereotactic injection of 2×105 firefly luciferase-expressing CT2A cells)[1]
Dosage: 2 mg/kg; 20 mg/kg
Administration: p.o.; 5 consecutive days per week; 4 weeks
Result: Significantly prolonged mouse survival at 20 mg/kg compared to vehicle control and TMZ (HY-17364) groups.
Showed 20 mg/kg dose was significantly more effective than 2 mg/kg dose at prolonging survival.
Made treated mice regain lost body weight more quickly than TMZ-treated mice following treatment cessation.
Animal Model: C57BL/6 (male, 6-8 weeks old, 20±2 g)[1]
Dosage: 2 mg/kg; 20 mg/kg; 66 mg/kg; 132 mg/kg
Administration: p.o.; daily; 7 days
Result: Caused no significant weight loss in any HJ03 dose group over 7-day treatment period.
Maintained white blood cell and lymphocyte counts within normal physiological ranges in 2, 20, and 66 mg/kg dose groups; induced significant decrease in white blood cell and lymphocyte counts below normal ranges only in 132 mg/kg dose group.
Kept red blood cell counts within normal ranges across all HJ03 dose groups.
Molecular Weight

482.75

Formula

C16H22Cl3N7O4
CAS No.
SMILES

ClCCNC(N(CCN(C1=CC=CC(Cl)=C1)CCN(C(NCCCl)=O)N=O)N=O)=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
References
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HJ03 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:

HJ033028123-48-7HJ 03HJ-03FerroptosisDNA Alkylator/CrosslinkerDNA/RNA SynthesisApoptosisReactive Oxygen Species (ROS)ferroptosiscolorectal cancerU87U251p53blood-brain barrierglioblastomaATF3SLC7A11DNA damageInhibitorinhibitorinhibit

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