protac rar degrader-1

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

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

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

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

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

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

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 Her3 Degrader-8 (Compound PP2) is a proteolysis targeting chimera (PROTAC) that degrades the Her3 protein in vitro and in cellular assays, with potential applications in investigating diseases modulated by HER family proteins [1].

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule from the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, it effectively degrades AR-V7 protein and induces apoptosis in prostate cancer (PC) cells, with degradation efficiencies of 62.2% (1 μM) and 71.1% (5 μM) in VCaP cells [1].

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].

PROTAC Axl Degrader 2, a potent and selective PROTAC Axl degrader, demonstrates an IC50 of 1.61 µM. It exhibits anti-proliferative and anti-migratory activities in vitro and induces mehuosis [1].

PROTAC IRAK4 Degrader-2 (Compound 9) is a PROTAC-based degrader that potently reduces IRAK4 levels, achieving a DC50 of 151 nM in peripheral blood mononuclear cells (PBMCs). It also notably decreases IRAK4 protein levels with a DC50 of 36 nM in the same cell type and inhibits several cytokines in PBMCs [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].

PROTAC pan-IAP degrader-1 (Compound 9) is a pan- IAP degrader PROTAC . PROTAC pan-IAP degrader-1 degrades XIAP , cIAP1 and cIAP2 with DC 50 s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1] .

PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2 and demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells.

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 BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC that acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1 Sirt3 (IC50s > 100 μM)[1].

PROTAC MDM2 Degrader-3 utilizes PROTAC technology to degrade MDM2 by combining a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

PROTAC CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

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

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

PROTAC TYK2 degrader-1 (CPD-155) functions as a selective degrader of TYK2, demonstrating a degradation maximum (D max) greater than 60%. (Structure Note: PINK, TYK2 ligand 1; Blue, VHL ligand Thalidomide; Black, linker). This compound effectively targets TYK2 for degradation, utilizing a linker to connect the TYK2 ligand with the VHL ligand Thalidomide, each color-coded for identification.