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Chemical Structure| 2070014-87-6 Chemical Structure| 2070014-87-6

Structure of MRT68921 HCl
CAS No.: 2070014-87-6

Chemical Structure| 2070014-87-6

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MRT68921 HCl is a selective inhibitor of ULK1 and ULK2 with IC50 0f 2.9 nM and 1.1 nM.

Synonyms: MRT68921 HCl

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Product Details of MRT68921 HCl

CAS No. :2070014-87-6
Formula : C25H35ClN6O
M.W : 471.04
SMILES Code : O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl
Synonyms :
MRT68921 HCl
MDL No. :MFCD30187515
InChI Key :SCEOGAWLKSVXHH-UHFFFAOYSA-N
Pubchem ID :121230974

Safety of MRT68921 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of MRT68921 HCl

Hedgehog

Isoform Comparison

Biological Activity

Target
  • Autophagy

    ULK2, IC50:1.1 nM

    ULK1, IC50:2.9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MEC-1 cells 10 µM 8 hours Immunoblot analysis of p62/SQSTM1 levels confirmed venetoclax-induced autophagy in MEC-1 cells. Cancers (Basel). 2021 Sep 10;13(18):4557
THP1-DiFluo hLC3 cells 1-25 µM 24 hours Assessed autophagy flux induced by venetoclax, showing venetoclax triggered autophagy in a concentration-dependent manner. Cancers (Basel). 2021 Sep 10;13(18):4557
Primary microglia 1, 10, or 30 µM 3 or 6 hours To test the inhibitory effect of MRT68921 on autophagy, results showed that MRT68921 at 30 µM for 3 hours reduced autophagosome degradation, while at 10 µM for 6 hours it reduced both autophagosome formation and degradation. Front Immunol. 2021 Jan 29;11:620602
MEC-1 cells 1 µM 24 hours MRT68921 inhibited autophagy, leading to increased p62/SQSTM1 levels. Cancers (Basel). 2021 Sep 10;13(18):4557
MOLM-13 SORE6+ cells 50-500 nM 24 hours Inhibition of ULK1/2 activity significantly reduced the resistance of SORE6+ cells to Ara-C Int J Mol Sci. 2024 Jan 4;25(1):646
LN229 cells 20 μM 5 hours Inhibits ULK1 activity, blocks autophagy and induces apoptosis J Cell Mol Med. 2022 Jul;26(14):3873-3890
MT330 cells 20 μM 5 hours Inhibits ULK1 activity, blocks autophagy and induces apoptosis J Cell Mol Med. 2022 Jul;26(14):3873-3890
mouse embryonic fibroblasts (MEFs) 1 μM 1 hour To evaluate the inhibition of ULK1 activity by MRT68921 and its effect on autophagy. Results showed that MRT68921 significantly reduced phosphorylation of ATG13 at serine 318 and blocked autophagic flux. J Biol Chem. 2015 May 1;290(18):11376-83

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.23mL

4.25mL

2.12mL

References

 

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