1041644-43-2

1041644-43-2 structure
1041644-43-2 structure
  • Name: Nec-4
  • Chemical Name: Nec-4
  • CAS Number: 1041644-43-2
  • Molecular Formula: C15H13ClFN3O
  • Molecular Weight: 305.73
  • Catalog: Signaling Pathways Apoptosis RIP kinase
  • Create Date: 2019-02-08 13:58:18
  • Modify Date: 2024-01-14 17:05:10
  • Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.

Name Nec-4
Description Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
Related Catalog
Target

IC50: 2.6 μM (RIP1)[1].

In Vitro Nec-4 (compound 9) is a slightly better competitor than 7 with a lower Ki value that is similar to R-3. Nec-4 is again a slightly better competitor than Rac-3 with Ki and IC50 values comparable to 7 (Nec-4: IC50=2.6±0.1 μM, Ki=0.46±0.05 μM; 7: IC50=10.7±1.8 μM, Ki=4.5±0.9 μM). Overall, all three compounds cross-compete with each other but Nec-4 is able to more effectively displace both 20 and 26 in comparison to the parent compounds Rac-3 and 7, respectively. This suggests that Nec-4 binding likely significantly overlaps with both the Nec-1 and the Nec-3 binding sites.
References

[1]. Maki JL, et al. Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1. Anal Biochem. 2012 Aug 15;427(2):164-74.

Molecular Formula C15H13ClFN3O
Molecular Weight 305.73
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