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Merck

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

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A propos de cet article

Formule empirique (notation de Hill) :
C29H25N3O4S
Numéro CAS:
Poids moléculaire :
511.59
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Nom du produit

ML385, ≥98% (HPLC)

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

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Quality Level

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.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Yuanyuan Bian et al.
Molecular medicine reports, 25(1) (2021-11-10)
Vitiligo is a depigmentation disease commonly seen in clinical practice, mainly involving loss of functional epidermal pigment cells and hair follicle melanocytes. Narrow‑band ultraviolet B (NB‑UVB) has emerged as the first choice of treatment for vitiligo, but long‑term exposure may have
Amy M Ehrlich et al.
BMC microbiology, 20(1), 357-357 (2020-11-24)
Bifidobacterium longum subsp. infantis (B. infantis) is a commensal bacterium that colonizes the gastrointestinal tract of breast-fed infants. B. infantis can efficiently utilize the abundant supply of oligosaccharides found in human milk (HMO) to help establish residence. We hypothesized that
Etay Ziv et al.
Radiology, 297(1), 225-234 (2020-08-12)
Background Intermediate stage hepatocellular carcinomas (HCCs) are treated by inducing ischemic cell death with transarterial embolization (TAE) or transarterial chemoembolization (TACE). A subset of HCCs harbor nuclear factor E2-related factor 2 (NRF2), a major regulator of the oxidative stress response
Yi Zhou et al.
Experimental and therapeutic medicine, 22(6), 1380-1380 (2021-10-16)
Hepatic ischemia-reperfusion injury (HIRI) is caused by blood flow recovery following ischemia. Baicalein (BAI), a natural antioxidant used in traditional Chinese medicine, eliminates excessive free radicals and protects the structure of the cell membrane. However, its protective mechanism against HIRI
Yanlian Xiong et al.
Stem cell research & therapy, 11(1), 468-468 (2020-11-06)
Mesenchymal stem cells (MSCs) were considered a regenerative therapeutic approach in both acute and chronic diseases. However, whether MSCs regulate the antioxidant metabolism of CD4+ T cells and weaken immunosenescence remains unclear. Here, we reported the protective effects of hPMSCs

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