der-4

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

PROTAC MDM2 Degrader-4, designed using PROTAC technology, combines a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase to degrade MDM2[1].

PROTAC BRM BRG1 degrader-4 (example 047) is a potent degrader targeting both BRM and BRG1, demonstrating DC50 values of 0.21 nM and 3.4 nM respectively in SW1573 cells.

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader, demonstrating DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively. It facilitates the ubiquitination and degradation of PARP1 and inhibits its enzymatic activity without causing significant DNA trapping effects. Additionally, PROTAC PARP1 degrader-4 can inhibit tumors with BRCA gene mutations while having minimal impact on the growth of normal cells.

PROTAC IRAK4 degrader-4 (US20190192668A1, compound I-127) is a Cereblon-based PROTAC specifically designed to target and degrade interleukin-1 receptor-associated kinase 4 (IRAK4).

PROTAC AR Degrader-4, an Androgen Receptor (AR) degrader, incorporates an IAP ligand binding group, a linker, and an AR binding group. It represents a class of degradation inducers known as specific and non-genetic IAP-dependent protein erasers (SNIPERs) [1], operating through a mechanism involving cIAP1.

PROTAC BRD9 Degrader-4 is a bifunctional degrader that targets BRD9, specifically designed for applications in cancer research.

PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].

PROTAC ERα Degrader-4, a highly potent and selective agent (K i: 5.08 μM), contains OBHSAs, a linker, and E3 ligase ligands. This compound demonstrates superb inhibitory effects and ERα degradation activity in both Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells, as well as in ERα-mutated BC cells. Additionally, PROTAC ERα Degrader-4 can induce apoptosis, making it valuable for cancer research.

PROTAC SMARCA2 4-degrader-4 (Compound I-434) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It efficiently degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM and degrades SMARCA4 in MV411 cells, also with a DC50 of less than 100 nM.

BRD9 Degrader-4 (BRD9c) is a bifunctional molecule that acts as an effective BRD9 degrader with a DC50 value of ≤25 nM. It exhibits anticancer properties.

PROTACSMARCA2 degrader-4 (Compound I-424) is a PROTAC degradative agent targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM and degrades SMARCA4 in MV411 with a DC50 exceeding 1 μM.