ML 385 - CAS 846557-71-9
Catalog number: B0084-007736
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H25N3O4S
Molecular Weight:
511.596
COA:
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Targets:
KEAP1-Nrf2
Description:
ML 385 is a novel and specific inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2; IC50 = 1.9 µM). ML 385 blocks NRF2 transcriptional activity, and enhances the efficacy of carboplatin as well as other chemotherapeutic drugs in lung cancer cells (NSCLC).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-007736 100 mg $399 In stock
B0084-007736 1 g $1450 In stock
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Brife Description:
Nrf2 inhibitor
Synonyms:
2-(1,3-benzodioxol-5-yl)-N-[5-methyl-4-[1-(2-methylbenzoyl)-2,3-dihydroindol-5-yl]-1,3-thiazol-2-yl]acetamide; ML-385
Solubility:
Soluble in DMSO.
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Density:
1.374±0.06 g/cm3
InChIKey:
LINHYWKZVCNAMQ-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
CC1=CC=CC=C1C(=O)N2CCC3=C2C=CC(=C3)C4=C(SC(=N4)NC(=O)CC5=CC6=C(C=C5)OCO6)C
1.Mechanisms of oxidative stress, apoptosis, and autophagy involved in graphene oxide nanomaterial anti-osteosarcoma effect.
Tang Z;Zhao L;Yang Z;Liu Z;Gu J;Bai B;Liu J;Xu J;Yang H Int J Nanomedicine. 2018 May 17;13:2907-2919. doi: 10.2147/IJN.S159388. eCollection 2018.
Background: ;Graphene and its derivative graphene oxide (GO) have been implicated in a wide range of anticancer effects.;Purpose: ;The objective of this study was to systematically evaluate the toxicity and underlying mechanisms of GO on two osteosarcoma (OSA) cancer cell lines, MG-63 and K;7;M;2; cells.;Methods: ;MG-63 and K;7;M;2; cells were treated by GO (0-50 µg/mL) for various time periods. Cell viability was tested by MTT and Live/Dead assays. A ROS Detection Kit based on DHE oxidative reaction was used for ROS detection. An Annexin V-FITC Apoptosis Kit was used for apoptosis detection. Dansylcadaverine (MDC) dyeing was applied for seeking unspecific autophagosomes. Western blot and Immunofluorescence analysis were used for related protein expression and location.;Results: ;K;7;M;2; cells were more sensitive to GO compared with MG-63 cells. The mechanism was attributed to the different extent of the generation of reactive oxygen species (ROS). In K;7;M;2; cells, ROS was easily stimulated and the apoptosis pathway was subsequently activated, accompanied by elevated expression of proapoptosis proteins (such as caspase-3) and decreased expression levels of antiapoptosis proteins (such as Bcl-2).
2.Isoliquiritigenin Ameliorates Acute Pancreatitis in Mice via Inhibition of Oxidative Stress and Modulation of the Nrf2/HO-1 Pathway.
Liu X;Zhu Q;Zhang M;Yin T;Xu R;Xiao W;Wu J;Deng B;Gao X;Gong W;Lu G;Ding Y Oxid Med Cell Longev. 2018 Apr 26;2018:7161592. doi: 10.1155/2018/7161592. eCollection 2018.
Oxidative stress plays a crucial role in the pathogenesis of acute pancreatitis (AP). Isoliquiritigenin (ISL) is a flavonoid monomer with confirmed antioxidant activity. However, the specific effects of ISL on AP have not been determined. In this study, we aimed to investigate the protective effect of ISL on AP using two mouse models. In the caerulein-induced mild acute pancreatitis (MAP) model, dynamic changes in oxidative stress injury of the pancreatic tissue were observed after AP onset. We found that ISL administration reduced serum amylase and lipase levels and alleviated the histopathological manifestations of pancreatic tissue in a dose-dependent manner. Meanwhile, ISL decreased the oxidative stress injury and increased the protein expression of the Nrf2/HO-1 pathway. In addition, after administering a Nrf2 inhibitor (ML385) or HO-1 inhibitor (zinc protoporphyrin) to block the Nrf2/HO-1 pathway, we failed to observe the protective effects of ISL on AP in mice. Furthermore, we found that ISL mitigated the severity of pancreatic tissue injury and pancreatitis-associated lung injury in a severe acute pancreatitis model induced by L-arginine. Taken together, our data for the first time confirmed the protective effects of ISL on AP in mice via inhibition of oxidative stress and modulation of the Nrf2/HO-1 pathway.
3.Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors.
Singh A;Venkannagari S;Oh KH;Zhang YQ;Rohde JM;Liu L;Nimmagadda S;Sudini K;Brimacombe KR;Gajghate S;Ma J;Wang A;Xu X;Shahane SA;Xia M;Woo J;Mensah GA;Wang Z;Ferrer M;Gabrielson E;Li Z;Rastinejad F;Shen M;Boxer MB;Biswal S ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. Epub 2016 Oct 17.
Loss of function mutations in Kelch-like ECH Associated Protein 1 (KEAP1), or gain-of-function mutations in nuclear factor erythroid 2-related factor 2 (NRF2), are common in non-small cell lung cancer (NSCLC) and associated with therapeutic resistance. To discover novel NRF2 inhibitors for targeted therapy, we conducted a quantitative high-throughput screen using a diverse set of ∼400 000 small molecules (Molecular Libraries Small Molecule Repository Library, MLSMR) at the National Center for Advancing Translational Sciences. We identified ML385 as a probe molecule that binds to NRF2 and inhibits its downstream target gene expression. Specifically, ML385 binds to Neh1, the Cap 'N' Collar Basic Leucine Zipper (CNC-bZIP) domain of NRF2, and interferes with the binding of the V-Maf Avian Musculoaponeurotic Fibrosarcoma Oncogene Homologue G (MAFG)-NRF2 protein complex to regulatory DNA binding sequences. In clonogenic assays, when used in combination with platinum-based drugs, doxorubicin or taxol, ML385 substantially enhances cytotoxicity in NSCLC cells, as compared to single agents. ML385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation, leading to gain of NRF2 function.
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CAS 846557-71-9 ML 385

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