RIPK3-IN-1 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

512.53

C₂₉H₂₅FN₄O₄

2361139-70-8

Solid

Light yellow to yellow

O=C(C1=CC=CN(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C(C)=C3C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [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.  [Content Brief]