PeptideDB

RIPK3-IN-1

CAS: 2361139-70-8 F: C29H25FN4O4 W: 512.53

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 o
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Bioactivity 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].
Target IC50: 9.1 nM (RIPK3), 5.5 μM (RIPK1), >10 μM (RIPK2)
Invitro 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].
Name RIPK3-IN-1
CAS 2361139-70-8
Formula C29H25FN4O4
Molar Mass 512.53
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.