DHODH-IN-33
DHODH-IN-33 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor with potent activity against A549 (IC50 = 5.22 μM) and 5637 (IC50 = 3.03 μM). DHODH-IN-33 induces autophagy-dependent ferroptosis (mitochondrial dysfunction, lipid peroxidation, and ROS accumulation) with no notable toxicity in vivo. DHODH-IN-33 exerts anti-cancer effect by promoting the autophagy-dependent degradation of DHODH. DHODH-IN-33 can be used for non-small cell lung cancer and bladder cancer.
For research use only. We do not sell to patients.
- CAS No.: 3026839-88-0
- Formula: C23H21NO4S
- Molecular Weight:407.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
DHODH-IN-33 (compound 3af) (48 h) exhibits potent activity against A549 (IC50 = 5.22 μM) and 5637 (IC50 = 3.03 μM)[1].
DHODH-IN-33 (5 and 10 μM, 48 h) does not induce A549 death via the apoptosis mechanism[1].
DHODH-IN-33 (5 and 10 μM, 24 h) links the induction of ferroptosis to the activation of autophagy in A549 cells, primarily through the coordinated degradation of redox-stabilizing enzymes[1].
DHODH-IN-33 (5 and 10 μM, 48 h) induces autophagy-dependent ferroptosis as the primary death pathway in A549 cells by initiating autophagy, inhibiting DHODH and lipid peroxidation, which together act as upstream switches to drive the downstream execution event of lipid peroxidation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:5, 10 μM
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Incubation Time:48 h
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Result:Exhibited 10.95% and 21.24% apoptosis at concentration of 5 μM and 10 μM, respectively.
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Cell Line:A549 cells
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Downregulated the expression of DHODH, but had little effect on the level of GPX4.
Increased the Beclin-1 and LC3 II (lipidated form) levels.
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Cell Line:A549 cells
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Concentration:5, 10 μM
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Incubation Time:48 h
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Result:Inhibited the cell viability of the A549 cells at various concentrations, particularly at a concentration of 10 μM.
Caused cytotoxicity can be reversed by 3-MA, Lip-1 and MitoQH2 with efficacy in the order of 3-MA > Lip-1 > MitoQH2.
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Cell Line:A549 cells
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Caused an upregulation of LC3 II and a downregulation of DHODH that were not significantly reversed by the addition of either the lipid peroxidation inhibitor Lip-1 or the DHODH enzyme substitute MitoQH2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (8 week-old)[1]
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Dosage:10 or 20 mg/kg
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Administration:i.p., once every 48 h for 14 days
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Result:Achieved tumor growth inhibition rates of 19.37% and 58.33% on day 14 at the corresponding doses of 10 mg/kg and 20 mg/kg, respectively.
Upregulated the expression level of LC3 II at administration of 20 mg/kg.
Increased ACSL4 protein.
Chemical Information
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CAS No. 3026839-88-0
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Molecular Weight 407.48
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Formula C23H21NO4S
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SMILES
COC1=CC2=C(N(C3C4=CC=CC=C4OC3C2)S(=O)(C5=CC=C(C=C5)C)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHODH-IN-33 Related Classifications
HY-179531 Related Classifications
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