PROTAC RAR Degrader-1

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].

Product Specifications

CAS Number

[1351169-27-1]

UNSPSC

12352005

Target

PROTACs; RAR/RXR; SNIPERs

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer; Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/protac-rar-degrader-1.html

Purity

97.91

Solubility

DMSO : ≥ 80 mg/mL

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

Molecular Formula

C51H72N4O11

Molecular Weight

917.14

References & Citations

[1]Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176.|[2]Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19 (22) :6768-78.