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| | PROTAC RAR Degrader-1 Basic information |
| Product Name: | PROTAC RAR Degrader-1 | | Synonyms: | PROTAC RAR Degrader-1;Benzoic acid, 2-[[(18S,21S,22R)-22-amino-21-hydroxy-18-(2-methylpropyl)-5,17,20-trioxo-23-phenyl-7,10,13-trioxa-4,16,19-triazatricos-1-yl]oxy]-4-[(1E)-3-[3,5-bis(1,1-dimethylethyl)phenyl]-3-oxo-1-propen-1-yl]-;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;2-(3-{2-[2-(2-{2-[(2S)-2-[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido]-4-methylpentanamido]ethoxy}ethoxy)ethoxy]acetamido}propoxy)-4-[(1E)-3-(3,5-di-tert-butylphenyl)-3-oxoprop-1-en-1-yl]benzoic acid | | CAS: | 1351169-27-1 | | MF: | C51H72N4O11 | | MW: | 917.14 | | EINECS: | | | Product Categories: | | | Mol File: | 1351169-27-1.mol |  |
| | PROTAC RAR Degrader-1 Chemical Properties |
| Boiling point | 1079.7±65.0 °C(Predicted) | | density | 1.160±0.06 g/cm3(Predicted) | | pka | 3.37±0.36(Predicted) | | form | Solid | | color | White to off-white |
| | PROTAC RAR Degrader-1 Usage And Synthesis |
| Uses | 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]. | | IC 50 | cIAP1; RXR α | | 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. DOI:10.1016/j.bmc.2011.09.041
[2] Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176. DOI:10.1016/j.csbj.2019.01.006 |
| | PROTAC RAR Degrader-1 Preparation Products And Raw materials |
| Raw materials | Ethanone, 1-[3,5-bis(1,1-dimethylethyl)phenyl]-2-bromo--->12,15,18-Trioxa-2,6,9,21-tetraazatetracosanoic acid, 24-[5-[(1E)-3-[3,5-bis(1,1-dimethylethyl)phenyl]-3-oxo-1-propen-1-yl]-2-(methoxycarbonyl)phenoxy]-4-hydroxy-7-(2-methylpropyl)-5,8,20-trioxo-3-(phenylmethyl)-, 9H-fluoren-9-ylmethyl ester, (3R,4S,7S)- |
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