| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H19N3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
MSU38225 is a selective Nrf2 inhibitor that increases ROS levels by suppressing antioxidant production. It arrests cells at the G2/M phase, enhances cellular sensitivity to chemotherapeutic agents, and acts synergistically with Carboplatin and 5-fluorouracil. It exhibits anticancer activity against lung cancer and can be used in research related to non-small cell lung cancer[1][2]. It is supplied as an off-white to light yellow solid (C21H19N3, MW 313.40) at 99.94% purity.
Physical & Chemical Properties
| CAS Number | 1629160-83-3 |
|---|---|
| Molecular Formula | C21H19N3 |
| Molecular Weight | 313.40 g/mol |
| Purity | 99.94% |
| 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 |
| Signaling Pathway | NF-κB; Metabolic Enzyme/Protease; Immunology/Inflammation |
| Solubility | In Vitro: DMSO: 100 mg/mL (319.08 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (319.08 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In MCF-7 NRF2/ARE reporter cells, MSU38225 (24 h) blocks tBHQ-induced Nrf2 transcriptional activity without causing cytotoxicity[1]. MSU38225 (24 h) lowers expression of downstream Nrf2 target genes and proteins in KEAP1-mutant A549 lung cancer cells, while NFE2L2 mRNA levels stay unchanged[1]. In tBHP-stimulated KEAP1-mutant A549 lung cancer cells, MSU38225 (24 h) raises ROS production in a dose-dependent manner through an Nrf2-dependent mechanism[1]. MSU38225 (72 h) suppresses cancer cell proliferation, with stronger potency in Nrf2-dependent KEAP1-mutant A549 and H460 lung cancer cells, acting through an Nrf2-dependent mechanism[1]. MSU38225 (7 days) has a significant, dose-dependent inhibitory effect on 3D colony formation by A549, H460 and A427 lung cancer cells in soft agar[1]. In KEAP1G12C-mutant A549 lung cancer cells, MSU38225 (72 h) synergistically strengthens the antiproliferative effects of Carboplatin and 5-fluorouracil[1]. In KEAP1-mutant non-small cell lung cancer cells (A549 and H460), MSU38225 (10 μM; 24 h) lowers NRF2 protein levels; it also significantly downregulates mRNA expression of NRF2 target genes (NQO1, GCLC, AKR1C2 and GCLM) in A549 cells[2]. After 12 h of low-serum synchronization, MSU38225 (10 μM; 24 h) causes G2/M phase arrest in KEAP1-mutant non-small cell lung cancer cells A549 and H460[2].
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) given alone does not statistically significantly slow A549 xenograft tumor growth; combined with carboplatin, it significantly reduces tumor growth while remaining well tolerated in Mus musculus[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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