R1-ICR-5

R1-ICR-5 is a selective PROTAC degrader that targets serine/threonine-protein kinase 1 (RIPK1) . R1-ICR-5 mediates the degradation of RIPK1 through VHL, thereby deregulating the TNFR1 and TLR3/4 signaling hubs, enhancing the output of NF-κB, MAPK, and IFN signaling, and simultaneously promoting the activation of RIPK3 and the induction of necroptosis. R1-ICR-5 is promising for research of cancers and inflammatory diseases. (Pink: PK68 (HY-128348) ; Black: linker (HY-W012241) ; Blue: (S, R, S) -AHPC (HY-125845) [1].

Product Specifications

CAS Number

[3070346-91-4]

UNSPSC

12352005

Target

NF-κB; p38 MAPK; PROTACs; Ser/Thr Kinase; TNF Receptor; Toll-like Receptor (TLR)

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB; PROTAC

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Purity

98.73

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(OC1CCCCC1)NC2=CC(C3=CC=C4N=C(NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O)=O)SC4=C3)=CN=C2C

Molecular Formula

C54H70N8O7S2

Molecular Weight

1007.31

References & Citations

[1]Mannion J, et al. A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death. Immunity. 2024 Jul 9;57 (7) :1514-1532.e15.