LD4172 is a selective RIPK1 PROTAC degrader with a Ki of 4.8 nM. LD4172 induces RIPK1 protein degradation via ternary complex formation with RIPK1 and VHL E3 ligase, driving ubiquitination and proteasomal breakdown. LD4172 abrogates TNF-induced classical NF-kappaB signaling in TRAF2-deficient cells, impairing IkappaBalpha phosphorylation and degradation, and reducing IL-8 production. LD4172 induces apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy. LD4172 acts as a chemical probe for investigating RIPK1 scaffolding functions. LD4172 can be used for the research of melanoma, colon cancer[1][2].
Molekulargewicht:
1149.37
Reinheit:
98.32
CAS Nummer:
[2782022-40-4]
Formel:
C61H75F3N10O7S
Target-Kategorie:
Apoptosis,PROTACs,RIP kinase
Anwendungsbeschreibung:
MCE Product type: Reference compound1
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
