SML1833

ML385

≥98% (HPLC), powder, Nrf2 transcription factor inhibitor

• Synonyme(s) : N-[4-[2,3-Dihydro-1-(2-methylbenzoyl)-1H-indol-5-yl]-5-methyl-2-thiazolyl]-1,3-benzodioxole-5-acetamide
• Formule empirique (notation de Hill) : C₂₉H₂₅N₃O₄S
• Numéro CAS: 846557-71-9
• Poids moléculaire : 511.59
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Propriétés

• Nom du produit: ML385, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: O=C(NC1=NC(C2=CC=C(N(C(C3=C(C)C=CC=C3)=O)CC4)C4=C2)=C(C)S1)CC5=CC(OCO6)=C6C=C5
• InChI: 1S/C29H25N3O4S/c1-17-5-3-4-6-22(17)28(34)32-12-11-20-15-21(8-9-23(20)32)27-18(2)37-29(31-27)30-26(33)14-19-7-10-24-25(13-19)36-16-35-24/h3-10,13,15H,11-12,14,16H2,1-2H3,(H,30,31,33)
• InChI key: LINHYWKZVCNAMQ-UHFFFAOYSA-N

Description

Biochem/physiol Actions

ML385 inihbits the activity of the Nrf2 transcription factor by binding to Neh1, a CNC-bZIP domain that allows Nrf2 to heterodimerize with small Maf proteins, blocking NRF2 transcriptional activity. Much research has been done on activating Nrf2 because it induces cytoprotective antioxidant genes. However, some cancer cells may use Nrf2 similarly for their survival. Nrf2 is overexpressed in certain cancers such as non-small cell lung cancer (NSCLC) often due to loss of function mutations in KEAP1, which targets Nrf2 for proteasomal degradation. ML385 was found to have anti-tumor activity with specificity and selectivity for NSCLC cells with KEAP1 mutations.

ML385 inihbits the activity of the Nrf2 transcription factor by binding to Neh1.

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable