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ML385

Catalog No.
B8300
NRF2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$78.00
In stock
10mg
$117.00
In stock
25mg
$247.00
In stock
50mg
$403.00
In stock
100mg
$637.00
In stock
200mg
$975.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

ML385 is a novel and specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM [1]. 

NRF2, a redox sensitive basic leucine zipper (bZIP) transcription factor, has emerged as the “master regulator” of cell survival through coordinated induction of cytoprotective antioxidant genes, phase-II detoxification enzymes, multidrug transporters, and central metabolic pathways. Gain-of-function mutations in NRF2 are common in non-small cell lung cancer (NSCLC), associated with therapeutic resistance [1]. 

In A549 cells, ML385 treatment at concentrations of 0 ~ 5 μM for 72 h dose-dependently reduced the expression levels of NRF2 and its target genes. At the concentration of 5 μM, a time-dependent decrease in NRF2 signaling could be observed in ML385-treated A549 cells, with the maximum decline at 72 h [1]. 

In mouse models of human NSCLC, single agent Carboplatin (5 mg/kg, q.d., i.p.) or ML385 (30 mg/kg, q.d., i.p.)-treated groups had 42% and 57% of their pretreatment lung volume at 3 weeks, respectively, while the antitumor and anti-metastatic effect of Carboplatin and ML385 combination treatment was significantly obvious with 74% lung volume retention at 3 weeks [1]. 

Reference:

[1]. Singh A, Venkannagari S, Oh K H, et al. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS Chemical Biology, 2016, 11(11): 3214-3225.

Chemical Properties

StorageStore at -20°C
M.Wt511.59
Cas No.846557-71-9
FormulaC29H25N3O4S
Solubility≥30mg/mL in DMSO
Chemical Name2-(benzo[d][1,3]dioxol-5-yl)-N-(5-methyl-4-(1-(2-methylbenzoyl)indolin-5-yl)thiazol-2-yl)acetamide
SDFDownload SDF
Canonical SMILESO=C(CC1=CC2=C(C=C1)OCO2)NC3=NC(C4=CC=C5N(CCC5=C4)C(C6=C(C=CC=C6)C)=O)=C(S3)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control