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.
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- No. CAS: 3028123-48-7
- Fòrmula: C16H22Cl3N7O4
- Peso molecular:482.75
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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.
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Cell Line:U251, U87, T98G
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Concentration:0.25, 0.5 andn 1 μM (U251); 1, 2 and 4 μM (U87); 2, 4 and 8 μM (T98G)
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Incubation Time:14 days
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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.
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Cell Line:U87
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Concentration:4, 8 and 16 μM
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Incubation Time:72 h
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Result:Induced U87 spheroid shrinkage and cell death at 4 μM.
Caused almost complete spheroid death at 16 μM.
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Cell Line:U251, U87, T98G
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Concentration:1, 2 and 4 μM (U251); 5 μM (U87)
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Incubation Time:48 h, 72 h
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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.
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Cell Line:U251, U87, T98G
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Concentration:1, 2 and 4 μM (U251); 5, 10 and 20 μM (U87); 10, 20 and 40 μM (T98G)
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Incubation Time:48 h, 72 h
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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.
| 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 |
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.
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Animal Model:C57BL/6 (male, 8 weeks old, intracranial stereotactic injection of 2×105 firefly luciferase-expressing CT2A cells)[1]
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Dosage:2 mg/kg; 20 mg/kg
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Administration:p.o.; 5 consecutive days per week; 4 weeks
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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.
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Animal Model:C57BL/6 (male, 6-8 weeks old, 20±2 g)[1]
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Dosage:2 mg/kg; 20 mg/kg; 66 mg/kg; 132 mg/kg
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Administration:p.o.; daily; 7 days
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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.
Chemical Information
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No. CAS 3028123-48-7
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Peso molecular 482.75
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Fòrmula C16H22Cl3N7O4
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SMILES
ClCCNC(N(CCN(C1=CC=CC(Cl)=C1)CCN(C(NCCCl)=O)N=O)N=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HJ03 Related Classifications
HY-181982 Related Classifications
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