2782022-40-4
Chemical Structure
LD4172
- CAS No.: 2782022-40-4
- Formula:C61H75F3N10O7S
- Molecular Weight:1149.37
IUPAC Name: N1-(3-(4-amino-5-(1-(2-(3-(trifluoromethoxy)phenyl)acetyl)indolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)-N12-((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)dodecanediamide
InChIKey: RMSGROMYBXPAFX-XVYCCKKLSA-N
SMILES: O=C(CC1=CC=CC(OC(F)(F)F)=C1)N2CCC3=C2C=CC(C4=CN(C5=NC=NC(N)=C45)CCCNC(CCCCCCCCCCC(N[C@H](C(N6C[C@@H](C[C@H]6C(N[C@H](C7=CC=C(C=C7)C8=C(N=CS8)C)C)=O)O)=O)C(C)(C)C)=O)=O)=C3
Biological Activity: 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-κB signaling in TRAF2-deficient cells, impairing IκBα 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LD4172 | 98.32% | 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-κB signaling in TRAF2-deficient cells, impairing IκBα 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. | ||||||||||||||||||||
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- [1]. Wagner J, et al. TRAF2 and RIPK1 redundantly mediate classical NFκB signaling by TNFR1 and CD95-type death receptors. Cell Death Dis. 2025;16(1):35. Published 2025 Jan 21. [Content Brief]
- [2]. Yu X, et al. Development of a RIPK1 degrader to enhance antitumor immunity. Nat Commun. 2024;15(1):10683. Published 2024 Dec 16. [Content Brief]
Keywords
