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1190379-70-4

1190379-70-4 structure
1190379-70-4 structure
  • Name: MRT67307
  • Chemical Name: MRT68921
  • CAS Number: 1190379-70-4
  • Molecular Formula: C25H34N6O
  • Molecular Weight: 434.577
  • Catalog: Signaling Pathways Autophagy ULK
  • Create Date: 2018-01-16 21:32:14
  • Modify Date: 2024-01-02 09:24:04
  • MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

Name MRT68921
Synonyms N-[3-({5-Cyclopropyl-2-[(2-methyl-1,2,3,4-tetrahydro-6-isoquinolinyl)amino]-4-pyrimidinyl}amino)propyl]cyclobutanecarboxamide
Cyclobutanecarboxamide, N-[3-[[5-cyclopropyl-2-[(1,2,3,4-tetrahydro-2-methyl-6-isoquinolinyl)amino]-4-pyrimidinyl]amino]propyl]-
MRT67307
Description MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
Related Catalog
Target

IC50: 2.9 nM (ULK1), 1.1 nM(ULK2)[1]

In Vitro ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nm) and greater than a 30-fold reduction for ULK2 (1.1 nm). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation[1].
Kinase Assay Kinase assays are carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and 0.1% β-mercaptoethanol, containing 30 μM cold ATP, and 0.5 μCi of [γ-32P]ATP for 5 min at 25 °C. Prior to ATP addition, reaction mixes are pre-warmed to 25 °C for 5 min. Reactions are stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot[1].
Cell Assay MEFs and 293T cells are grown in DMEM, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37°C, 5% CO2. For induction of autophagy, cells are typically grown to 75% confluency, ished twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control). MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) is included[1].
References

[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83.

Density 1.3±0.1 g/cm3
Molecular Formula C25H34N6O
Molecular Weight 434.577
Exact Mass 434.279419
LogP 2.20
Index of Refraction 1.659
Storage condition 2-8℃