fkbp12 protac dtag7

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.

PROTAC ERα Degrader-7 (Compound i-320) is a powerful PROTAC degrader targeting the estrogen receptor alpha (ERα), exhibiting a DC50 of 0.000006 µM. This compound consists of a cereblon-binding segment, LBM, connected to ERBM, an ERα-binding ligand that includes a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring [1].

PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1].

PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC that links von Hippel-Lindau and BRD4 ligands. When conjugated with STEAP1 and CLL1 antibodies, this compound effectively degrades BRD4 protein in PC3 prostate cancer cells, demonstrating potent activity with DC50 values of 0.39 nM and 0.24 nM, respectively [1].

PROTAC IRAK4 degrader-7 (Compound I-417) is an orally administered agent with antitumor properties, functioning as a PROTAC IRAK4 degrader [1].

PROTAC BRD4 Degrader-7, a potent bromodomain BRD4 inhibitor exemplified by compound 1a, demonstrates half-maximal inhibitory concentrations (IC50s) of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively [1].

FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

PROTAC FKBP Degrader-3 is a potent FKBP degrader, consisting of a FKBP ligand binding group, a linker, and a VHL binding group [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R T790M degrader with a DC50 of 13.2 nM. It effectively inhibits NCI-H1975 cell proliferation with an IC50 of 46.82 nM, induces apoptosis, and causes G2 M phase arrest. This compound shows antitumor activity and is applicable in non-small cell lung cancer (NSCLC) research.

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting agent targeting EGFR L858R T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI-H1975 cells with an IC50 of 46.82 nM and significantly induces apoptosis and G2 M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].