1. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Keap1-Nrf2 Reactive Oxygen Species (ROS)
  3. MSU38225

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.

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

MSU38225

MSU38225 Chemical Structure

CAS No. : 1629160-83-3

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10 mM * 1 mL in DMSO
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Description

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[1][2].

In Vitro

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.

Cell Proliferation Assay[2]

Cell Line: A549 human lung cancer cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Inhibited cell proliferation by 9.8% relative to the vehicle control.

Western Blot Analysis[2]

Cell Line: A549 and H460 KEAP1-mutant non-small cell lung cancer cells
Concentration: 10 μM
Incubation Time: 24 h
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.

Cell Migration Assay [2]

Cell Line: A549 human lung cancer cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly reduced (p < 0.0001) cell migration by 65% relative to vehicle control.
In Vivo

MSU38225 (50 mg/kg; i.p.; twice daily; 4 weeks) alone does not statistically significantly slow A549 xenograft tumor growth, but in combination with carboplatin, it significantly reduces tumor growth while maintaining good tolerability in Mus musculus[1].

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

Animal Model: athymic nude mice (male, 6 weeks-old)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily; 4 weeks
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.
Molecular Weight

313.40

Formula

C21H19N3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=C(NC2=CC(C)=CC(C)=C2)N=C(C)C(C3=CC=CC=C3)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1908 mL 15.9541 mL 31.9081 mL
5 mM 0.6382 mL 3.1908 mL 6.3816 mL
View the 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.

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Purity & Documentation
References

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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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.

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MSU38225
Cat. No.:
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