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2361139-70-8

2361139-70-8 structure
2361139-70-8 structure
  • Name: RIPK3-IN-1
  • Chemical Name: RIPK3-IN-1
  • CAS Number: 2361139-70-8
  • Molecular Formula: C29H25FN4O4
  • Molecular Weight: 512.53
  • Catalog: Signaling Pathways Apoptosis RIP kinase
  • Create Date: 2020-08-07 17:54:47
  • Modify Date: 2024-01-13 19:19:53
  • RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM[1].

Name RIPK3-IN-1
Description RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM[1].
Related Catalog
Target

IC50: 9.1 nM (RIPK3), 5.5 μM (RIPK1), >10 μM (RIPK2)[1]

In Vitro RIPK3-IN-1 (Compound 18) also inhibits ABL, BRAF/V599E, MAP4K3, and SRC with IC50s of 0.37, 0.15, 0.012, and 0.075 μM, respectively[1]. Necroptosis is a programmed form of cell death and has been associated with a variety of diseases, including ischemia reperfusion injury, neurodegenerative disorders, pancreatic cancer, and autoimmune diseases such as inflammatory bowel disease (IBD). Upon stimulation of death receptors (such as the family of TNF receptors), signaling can initiate a necroptotic cell death process. This involves formation of a necrosome, which includes receptor interacting protein kinases 1 and 3 (RIPK1, RIPK3) in a cytosolic complex[1].
References

[1]. Amy C Hart, et al. Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage. ACS Med Chem Lett. 2019 May 6;11(3):266-271.

Molecular Formula C29H25FN4O4
Molecular Weight 512.53