Basic information Safety Supplier Related

ML385

Basic information Safety Supplier Related

ML385 Basic information

Product Name:
ML385
Synonyms:
  • ML385
  • CS-2542
  • ML 385; ML-385
  • N-[4-[2,3-Dihydro-1-(2-methylbenzoyl)-1H-indol-5-yl]-5-methyl-2-thiazolyl]-1,3-benzodioxole-5-acetamide
  • 2-(1,3-benzodioxol-5-yl)-N-[5-methyl-4-[1-(2-methylbenzoyl)-2,3-dihydroindol-5-yl]-1,3-thiazol-2-yl]acetamide
  • 1,3-Benzodioxole-5-acetamide, N-[4-[2,3-dihydro-1-(2-methylbenzoyl)-1H-indol-5-yl]-5-methyl-2-thiazolyl]-
  • Ferroptosis,ML385,Inhibitor,inhibit,ML-385,Keap1-Nrf2,ML 385
  • ML38
CAS:
846557-71-9
MF:
C29H25N3O4S
MW:
511.59
Product Categories:
  • api
Mol File:
846557-71-9.mol
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ML385 Chemical Properties

Density 
1.374±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO:31.4(Max Conc. mg/mL);61.38(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);58.64(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.49(Max Conc. mM)
form 
powder
pka
8.92±0.50(Predicted)
color 
white to beige
InChIKey
LINHYWKZVCNAMQ-UHFFFAOYSA-N
SMILES
O1C2=CC=C(CC(NC3=NC(C4C=CC5=C(C=4)CCN5C(=O)C4=CC=CC=C4C)=C(C)S3)=O)C=C2OC1
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ML385 Usage And Synthesis

Uses

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

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.

in vivo

ML385 in combination with carboplatin leads to a significant reduction in tumor cell proliferation, demonstrated by fewer Ki-67 positive cells. Tumor samples treated with ML385 show a significant reduction in NRF2 protein level and its downstream target genes[1]. ML385 (intraperitoneal injection; 30 mg/kg; 7 days) weakens the therapeutic effects of MSC-Exo on inflammation-induced astrocytic activation (e.g., reduced reactive astrogliosis, NF-κB deactivation) in mice[3].

Animal Model:8-week-old C57B/6 male mice[3]
Dosage:30 mg/kg; 7 days
Administration:Intraperitoneal injection
Result:Reversed inhibition of MSC-Exo on hippocampal astrocytic activation in vivo.

storage

Store at -20°C

References

[1] Singh A, et al. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225. DOI:10.1021/acschembio.6b00651
[2] Xinnong Liu, et al. Isoliquiritigenin ameliorates acute pancreatitis in mice via inhibition of oxidative stress and modulation of the Nrf2/HO-1 pathway. Oxid Med Cell Longev. 20 March 2018.
[3] Xian P, et al. Mesenchymal?stem?cell-derived?exosomes?as a?nanotherapeutic?agent?for?amelioration?of?inflammation-induced?astrocyte?alterations?in?mice.Theranostics.?2019 Aug 14;9(20):5956-5975. DOI:10.7150/thno.33872

ML385Supplier

Shanghai Chaolan Chemical Technology Center Gold
Tel
021-QQ：65489617 15618227136
Email
Sales@ATKchemical.com
Hefei Hirisun Pharmatech Co., Ltd. Gold
Tel
+86-0551-62678551 +86-15056975894
Email
sales@hirisunpharm.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Beijing HwrkChemical Technology Co., Ltd
Tel
18515581800 18501085097
Email
sales.bj@hwrkchemical.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
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