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PT-179 is an orthogonal Thalidomide (M2225) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. PT-179 (1-10 μM; 24 h) can induce eGFP degradation in HEK293T cells. The higher the evolution degree of the degron variant, the stronger the degradation efficiency of the corresponding tagged protein. SD40 is a degradation tag specific for PT-179. PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms.
| Molecular Weight | 343.33 |
| Formula | C17H17N3O5 |
| CAS Number | 2924858-25-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ligand for E3 Ligase Products |
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| OICR-8268
OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can be used in the development of DCAF1-based PROTACs. |
| BC-1215
BC-1215 is a novel inhibitor of F-box protein 3 (Fbxo3) activity. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 relieves allodynia by preventing ubiquitination-dependent Fbxl2/TRAF2/TNIK/pGluR1 signaling. BC-1215 exerted robust therapeutic effects in cytokine-driven inflammation, including pseudomona-induced lung injury and cecum ligation/punctured-induced sepsis, by targeting Fbxo3/Fbxl2/TRAF-mediated cytokine release. BC-1215 can be used for the research of inflammation. |
| VH 101, acid
VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. |
| (S,R,S)-AHPC-Boc
(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| Lenalidomide-Br
Lenalidomide-Br is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. |
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Products are for research use only. Not for human use. We do not sell to patients.
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