1351169-27-1
Chemical Structure
PROTAC RAR Degrader-1
- CAS No.: 1351169-27-1
- Formula:C51H72N4O11
- Molecular Weight:917.14
IUPAC Name: 2-(((18S,21S,22R)-22-amino-21-hydroxy-18-isobutyl-5,17,20-trioxo-23-phenyl-7,10,13-trioxa-4,16,19-triazatricosyl)oxy)-4-((E)-3-(3,5-di-tert-butylphenyl)-3-oxoprop-1-en-1-yl)benzoic acid
InChIKey: ZAOSGDCLGNWLSI-ACALULJJSA-N
SMILES: O=C(O)C1=CC=C(/C=C/C(C2=CC(C(C)(C)C)=CC(C(C)(C)C)=C2)=O)C=C1OCCCNC(COCCOCCOCCNC([C@H](CC(C)C)NC([C@@H](O)[C@H](N)CC3=CC=CC=C3)=O)=O)=O
Biological Activity: PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134))[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PROTAC RAR Degrader-1 | 97.91% | PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)). | ||||||||||||||||||||
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References
- [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78. [Content Brief]
- [2]. Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176. [Content Brief]
