protac brd-4 degrader-3

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.

PROTACBRD4 Degrader-32 (Compound 22) is a potent BRD4 PROTAC degrader with a DC50 of 0.20 nM. It employs a unique carbon-carbon linker to connect the BRD4 binding domain with the CRBN binding domain, forming a ternary complex that induces BRD4 ubiquitination and facilitates proteasomal degradation. PROTACBRD4 Degrader-32 holds promise for research into BRD4-related cancers, such as hematological malignancies.

PROTACBRD4 Degrader-33 is an enzyme-activated, click-responsive BRD4 PROTAC degrader designed with effective tumor microenvironment responsiveness. This compound exhibits exceptional penetration into tumor tissues and effectively inhibits PD-L1 protein expression. In the 4T1 tumor mouse model, PROTACBRD4 Degrader-33 demonstrates potent antitumor immunomodulatory activity.

PROTACBRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 values of 164 nM at 4 hours and 80 nM at 24 hours. It effectively degrades BRD4 within cells and exhibits long-lasting degradation kinetics.

PROTACBRD4 Degrader-35 (Compound 17) is a PROTAC degrader targeting BRD4. It is utilized in cancer research.

PROTACBRD4 Degrader-34 is a selective BRD4 PROTAC degrader (pDC50= 8.4) that induces VHL-mediated BD2 degradation and is applicable for cancer research.

PROTACBRD4 Degrader-36 (Compound TrimTAC-1) is a BRD4 PROTAC degrader. It has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. Additionally, PROTACBRD4 Degrader-36 exhibits cytotoxicity towards PANC-1 cells with a GI50 of 0.103 μM. This compound is applicable for tumor research.

PROTACBRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50 values of 86 nM and 106 nM for the short and long BRD4 isoforms, respectively. It significantly induces BRD4 degradation through covalent binding at the C232 site of the E3 ligase TRIM28.

PROTACBRD4 Degrader-37 is a PROTACBRD4 degrader with a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. It exhibits cytotoxicity against PANC-1 cells with a GI50 of 0.282 μM. PROTACBRD4 Degrader-37 is applicable for cancer research.

BTR2004 is a selective PROTAC degrader targeting the BET family (BRD2/3/4) proteins. It facilitates the formation of a ternary complex with BRD proteins and KLHL20, leading to ubiquitination and proteasomal degradation via the UPS pathway. BTR2004 shows potential for research in PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.