BTR2004

BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+) -JQ1-OH (HY-161125) ; Blue: BTR2000 (HY-172563) ; Black: Linker (HY-W015236) [1][2].

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Related Pathways

Epigenetics; PROTAC

Field of Research

Cancer

Smiles

CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCC(NCC(NCC(N[C@H](C(N5[C@H](C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CSC6)=O)=O)=O)CCC5)=O)CSCC7=CC=CC6=C7)=O)=O)=O)=O

Molecular Formula

C54H66ClN13O11S3

Molecular Weight

1204.83

References & Citations

[1]Farrell BM, et al. A synthetic KLHL20 ligand to validate CUL3KLHL20 as a potent E3 ligase for targeted protein degradation. Genes Dev. 2022 Sep 1;36 (17-18) :1031-1042.|[2]Fechtmeyer PH, et al. Temporal and Spatial Characterization of CUL3KLHL20-driven Targeted Degradation of BET family, BRD Proteins by the Macrocycle-based Degrader BTR2004. bioRxiv [Preprint]. 2024 Dec 7:2024.12.07.627262.