MSU38225
Based on 1 Customer Validation
MSU38225 is a selective Nrf2 inhibitor. MSU38225 increases ROS levels by inhibiting antioxidant production. MSU38225 arrests cells at the G2/M phase, enhances cellular sensitivity to chemotherapeutic agents, and exerts synergistic effects with Carboplatin (HY-17393) and 5-fluorouracil (HY-90006). MSU38225 exhibits anticancer activity against lung cancer. MSU38225 can be used in research related to non-small cell lung cancer.
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- Purity: 99.94%
- CAS No.: 1629160-83-3
- 화학식: C21H19N3
- 분자량:313.40
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Antioxidant Compound Library
HY-L037
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Oxygen Sensing Compound Library
HY-L045
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Ferroptosis Compound Library
HY-L051
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Cancer Metabolism Compound Library
HY-L083
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Transcription Factor-Targeted Library
HY-L090
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Anti-Colorectal Cancer Compound Library
HY-L103
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Anti-Ovarian Cancer Compound Library
HY-L173
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Radioprotector Library
HY-L178
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Fibrosis Compound Library
HY-L185
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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NF-κB Signaling Compound Library
HY-L014
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Stem Cell Signaling Compound Library
HY-L017
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
Biological Activity
MSU38225 (24 h) inhibits tBHQ-induced Nrf2 transcriptional activity in MCF-7 NRF2/ARE reporter cells without cytotoxicity[1].
MSU38225 (24 h) suppresses the expression of Nrf2 downstream target genes and proteins in KEAP1-mutant A549 lung cancer cells without altering NFE2L2 mRNA levels[1].
MSU38225 (24 h) increases ROS production in tBHP-stimulated KEAP1-mutant A549 lung cancer cells in a dose-dependent manner via an Nrf2-dependent mechanism[1].
MSU38225 (72 h) inhibits the proliferation of cancer cells; it exerts stronger potency in Nrf2-dependent KEAP1-mutant A549 and H460 lung cancer cells via an Nrf2-dependent mechanism[1].
MSU38225 (7 days) exerts a dose-dependent and significant inhibitory effect on the 3D colony formation of A549, H460 and A427 lung cancer cells in soft agar[1].
MSU38225 (72 h) synergistically enhances the antiproliferative effects of Carboplatin (HY-17393) and 5-fluorouracil (HY-90006) in KEAP1G12C-mutant A549 lung cancer cells[1].
MSU38225 (10 μM; 24 h) reduces NRF2 protein levels in KEAP1-mutant non-small cell lung cancer cells A549 and H460, and significantly downregulates the mRNA expression of NRF2 target genes NQO1, GCLC, AKR1C2 and GCLM in A549 cells[2].
MSU38225 (10 μM; 24 h) arrests KEAP1-mutant non-small cell lung cancer cells A549 and H460 at the G2/M phase following 12 h of low-serum synchronization[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human lung cancer cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Inhibited cell proliferation by 9.8% relative to the vehicle control.
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Cell Line:A549 and H460 KEAP1-mutant non-small cell lung cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Decreased NRF2 protein levels in A549 and H460 cells.
Significantly reduced mRNA levels of NRF2 target genes NQO1, GCLC, AKR1C2, and GCLM in A549 cells relative to vehicle control.
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Cell Line:A549 human lung cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly reduced (p < 0.0001) cell migration by 65% relative to vehicle control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude mice (male, 6 weeks-old)[1]
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Dosage:50 mg/kg
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Administration:i.p.; twice daily; 4 weeks
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Result:Slowed tumor growth, though the change was not statistically significant.
Significantly slowed tumor growth when combined with carboplatin compared to vehicle control (p<0.01) and carboplatin alone (p<0.05).
Decreased Nrf2 protein expression in tumors compared to vehicle control.
Showed good tolerability with no changes in mouse body weight over time.
Chemical Information
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CAS No. 1629160-83-3
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Appearance Solid
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분자량 313.40
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화학식 C21H19N3
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Color Off-white to light yellow
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SMILES
N#CC1=C(NC2=CC(C)=CC(C)=C2)N=C(C)C(C3=CC=CC=C3)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (319.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhang D, et al. A Novel Nrf2 Pathway Inhibitor Sensitizes Keap1-Mutant Lung Cancer Cells to Chemotherapy. Molecular cancer therapeutics. 2021 Sep;20(9):1692-1701. [Content Brief]
[2]. Hou Z, et al. Exploring structural effects in a new class of NRF2 inhibitors. RSC Med Chem. 2022 Nov 16;14(1):74-84. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL | 79.7703 mL |
| 5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL | 15.9541 mL | |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1908 mL | 7.9770 mL | |
| 15 mM | 0.2127 mL | 1.0636 mL | 2.1272 mL | 5.3180 mL | |
| 20 mM | 0.1595 mL | 0.7977 mL | 1.5954 mL | 3.9885 mL | |
| 25 mM | 0.1276 mL | 0.6382 mL | 1.2763 mL | 3.1908 mL | |
| 30 mM | 0.1064 mL | 0.5318 mL | 1.0636 mL | 2.6590 mL | |
| 40 mM | 0.0798 mL | 0.3989 mL | 0.7977 mL | 1.9943 mL | |
| 50 mM | 0.0638 mL | 0.3191 mL | 0.6382 mL | 1.5954 mL | |
| 60 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3295 mL | |
| 80 mM | 0.0399 mL | 0.1994 mL | 0.3989 mL | 0.9971 mL | |
| 100 mM | 0.0319 mL | 0.1595 mL | 0.3191 mL | 0.7977 mL |
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