In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ML385 is a novel and specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM .
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 .
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 .
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 .
. 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.
|Storage||Store at -20°C|
|Solubility||≥30mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For 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.|