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SML1644

Sigma-Aldrich

MRT68921 dihydrochloride

≥98% (HPLC)

Synonyme(s) :

N-[3-[[5-Cyclopropyl-2-[(1,2,3,4-tetrahydro-2-methyl-6-isoquinolinyl)amino]-4-pyrimidinyl]amino]propyl]-cyclobutanecarboxamide dihydrochloride

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About This Item

Formule empirique (notation de Hill):
C25H34N6O · 2HCl
Numéro CAS:
1190379-70-4
Poids moléculaire :
507.50
Code UNSPSC :
12352200
ID de substance PubChem :
329825985
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

H2O: 20 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

CN(C1)CCC2=C1C=CC(NC3=NC=C(C4CC4)C(NCCCNC(C5CCC5)=O)=N3)=C2.[H]Cl.[H]Cl

InChI

1S/C25H34N6O.2ClH/c1-31-13-10-19-14-21(9-8-20(19)16-31)29-25-28-15-22(17-6-7-17)23(30-25)26-11-3-12-27-24(32)18-4-2-5-18;;/h8-9,14-15,17-18H,2-7,10-13,16H2,1H3,(H,27,32)(H2,26,28,29,30);2*1H

Clé InChI

NLKPLTWKINJHCK-UHFFFAOYSA-N

Application

MRT68921 dihydrochloride has been used:
  • as a specific inhibitor of Unc-51-like kinase 1 (ULK1) in SH-SY5Y neuroblastoma cells
  • as an inhibitor of ULK1 and ULK2 kinases in intrahepatic lymphocytes
  • as a ULK1 inhibitor to test its effect on attenuation of autophagosome accumulation in ubiquitin-specific peptidase 24 (USP24) knockdown containing human neuroglioma H4 cells

Actions biochimiques/physiologiques

MRT68921 is a cell penetrant, potent and specific inhibitor of ULK1 and ULK2 kinases in vitro, which reduces ULK1 activity in cells and blocks autophagy induction. MRT68921 blocks mTOR dependent autophagy.
MRT68921 is cytotoxic and acts on oxidative stress signals to kill cancer cells, making it an effective tumor therapy agent.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Yiran Chen et al.
Cell death & disease, 11(8), 712-712 (2020-09-03)
Utilizing oxidative stress has recently been regarded as a potential strategy for tumor therapy. The NUAK family SNF1-like kinase 1 (NUAK1) is a critical component of the antioxidant defense system and is necessary for the survival of tumors. Therefore, NUAK1
Leo Swadling et al.
Cell reports, 30(3), 687-698 (2020-01-23)
Tissue-resident memory T cells have critical roles in long-term pathogen and tumor immune surveillance in the liver. We investigate the role of autophagy in equipping human memory T cells to acquire tissue residence and maintain functionality in the immunosuppressive liver environment. By
Julia A Thayer et al.
Autophagy, 16(1), 140-153 (2019-04-09)
Recent studies indicate a causative relationship between defects in autophagy and dopaminergic neuron degeneration in Parkinson disease (PD). However, it is not fully understood how autophagy is regulated in the context of PD. Here we identify USP24 (ubiquitin specific peptidase
Yasuomi Urano et al.
Autophagy, 14(11), 1943-1958 (2018-08-17)
PARK7/DJ-1 is a Parkinson disease- and cancer-associated protein that functions as a multifunctional protein involved in gene transcription regulation and anti-oxidative defense. Although PARK7 lacks the secretory signal sequence, it is secreted and plays important physiological and pathophysiological roles. Whereas
Anna M Schläfli et al.
Scientific reports, 11(1), 9011-9011 (2021-04-29)
ALK inhibitors effectively target EML4-ALK positive non-small cell lung cancer, but their effects are hampered by treatment resistance. In the present study, we asked whether ALK inhibition affects autophagy, and whether this may influence treatment response. Whereas the impact of

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