protac brd-4 degrader-5

PROTAC BRD4 Degrader-5 is a PROTAC-based compound that efficiently degrades BRD4 in both HER2-positive and HER2-negative breast cancer cell lines[1].

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

Homo-PROTAC pVHL30 degrader 1 is a potent PROTAC-based degrader of pVHL30.

PROTAC AR AR-V7 degrader-1 (27c) serves as a dual degrader targeting both AR and AR-V7, showcasing DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. It effectively induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) [1].

PROTAC ATR degrader-1 (compound ZS-7) serves as a powerful PROTAC degrader targeting ataxia telangiectasia and Rad3-related (ATR), exhibiting a DC50 of 0.53 μM. This compound is significant in the field of cancer research [1].

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [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 BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, used in cancer research.

PROTAC HSP90 degrader BP3 potently and selectively degrades HSP90 through a CRBN-dependent mechanism. It effectively diminishes HSP90 protein levels in MCF-7 cells with a half-maximal degradation concentration (DC50) of 0.99 µM. Additionally, this compound impedes the proliferation of breast cancer cells [1].

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].

PROTAC STING Degrader-1 (Compound SP23) is a STING-targeted PROTAC degrader with a DC50 of 3.2 μM, demonstrating anti-inflammatory activity [1].

PROTAC RIPK degrader-6 (example 1) is a PROTAC engineered for RIP Kinase degradation, comprising a RIP2 kinase inhibitor linked to a cereblon binder[1].

PROTAC Axl Degrader 1 is a potent and selective compound with an IC50 of 0.92 µM, exhibiting in vitro anti-proliferative and anti-migratory activities, and inducing mehuosis [1].

PROTAC BRD4 Degrader-11 (compound 9a), a PROTAC linked through ligands to von Hippel-Lindau and BRD4, effectively targets and degrades the BRD4 protein in PC3 prostate cancer cells when conjugated with STEAP1 and CLL1 antibodies, exhibiting potent activity with DC50 values of 0.23 nM and 0.38 nM for the respective conjugations [1].

PROTAC EZH2 Degrader-1 (Compound 150d) is a potent inhibitor that effectively suppresses EZH2 methyltransferase activity, with an IC50 of 2.7 nM. EZH2 plays a critical role in various tumorigenesis and development processes [1].

PROTAC BTK Degrader-2, a potent degrader of BTK through the PROTAC mechanism, effectively diminishes BTK protein levels [1].

PROTAC PD-1 PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1 PD-L1 PROTAC that effectively inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B OS-8 hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

PROTAC MDM2 Degrader-1 is a chemical compound that employs PROTAC technology to degrade MDM2, comprising a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC BRD2 BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.

PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.

PROTAC SMARCA2 degrader-3, a degrader targeting the SWI SNF ATPase subunits specifically SMARCA2, exhibits anticancer properties (WO2023244764A1; Compound 153) [1].

PROTAC ERα Y537S degrader-1 consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group, functioning as an estrogen receptor-alpha (ERα) Y537S degrader [1].

PROTAC BRD3 BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].

PROTAC BRD9 Degrader-6, with an IC50 value of 0.13 nM, is a potent degrader of BRD9 suitable for research on BAF complex-related disorders [1].

PROTAC CYP1B1 Degrader-1 (Compound 6C), an α-naphthoflavone chimera derivative, effectively targets and degrades cytochrome P450 (CYP) 1B1 to overcome agent resistance, displaying half-maximal inhibitory concentrations (IC50s) of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2. This compound is suitable for investigating prostate cancer characterized by overexpression of CYP1B1 [1].

PROTAC ATR degrader-2 (Compound 8i) serves as a PROTAC degrader targeting ATR, effectively degrading it in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, with DC50 values of 22.9 and 34.5 nM, respectively. This compound induces apoptosis and inhibits the proliferation of AML cells. Additionally, PROTAC ATR degrader-2 demonstrates favorable pharmacokinetic properties and potent antitumor activity in a mouse model of AML. (Pink: ATR ligand; Blue: E3 ligase ligand Lenalidomide; Black: linker) [1]

PROTAC CDK9 Degrader-1 is a selective degrader of cyclin-dependent kinase 9 (CDK9).

PROTAC BRD4 Degrader-21 (Comp 74), a potent BRD4 degrader, has shown significant inhibition of tumor growth in mouse xenograft models, indicating its potential for anticancer research [1].

PROTAC TG2 degrader-2 (compound 7) is a selective competitive degrader of Transglutaminase 2 (TG2) with a dissociation constant (Kd) greater than 100 μM. It inhibits cell migration and reduces TG2 levels in ovarian cancer cells, making it a valuable tool for ovarian cancer research [1].

PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent Protein Tyrosine Phosphatase Non-receptor Type 2 (PTPN2) degrader with potential applications in cancer and metabolic disease research [1].

PROTAC eDHFR Degrader-1 is a potent compound targeting and degrading eDHFR-YFP and various proteins of interest (POIs), such as YFP and Luciferase [1].

PROTAC BRD9 Degrader-2 is a bifunctional compound engineered for the targeted degradation of BRD9 (Bromodomain containing 9) in cancer research applications.

PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM.

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

PROTAC BRD4 Degrader-19 (compound 176) is a proteolysis-targeting chimera (PROTAC) developed to specifically degrade the BRD4 protein, potentially useful in cancer research [1].

PROTAC IRAK4 degrader-5 is a Cereblon-based compound designed to selectively degrade IRAK4.

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