protac erra ligand 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 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.

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.

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

PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

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

(rel)-PROTAC ERRα Degrader-1, a relative configuration of PROTAC ERRα Degrader-1, is an estrogen-related receptor alpha (ERRα) degrader comprising an MDM2 ligand binding moiety, a linker, and an ERRα binding moiety [1].

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

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].

BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation.

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).

K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells [1].

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. This thiadiazole-dioxide ligand suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.

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.

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

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.

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 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 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].

TSPO Ligand-Linker Conjugates 1, comprising a translocator protein (TSPO) ligand and a linker, is instrumental in synthesizing mitochondria-targeting autophagy-targeting chimera (AUTAC). This compound binds TSPO on the outer mitochondrial membrane (OMM), facilitating the degradation of malfunctioning mitochondria and proteins through mitophagy, thereby enhancing mitochondrial function. It holds potential applications in research related to mitochondrial dysfunction, encompassing neurodegenerative diseases, cancer, and diabetes [1].

TEAD ligand 1 is a ligand for the target protein TEAD. TEAD ligand 1 can be utilized in the synthesis of the PROTACTEAD degrader-1.

PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].

TSPO ligand-1 has affinity for peripheral and central benzodiazepine receptors.TSPO ligand-1 is an AUTAC4-binding protein in the transmembrane domain of the outer mitochondrial membrane, which induces mitochondrial autophagy and promotes intracellular mitochondrial regeneration.TSPO ligand-1 is involved in intracellular cholesterol transport, and can be used as a biomarker for brain injury and neurodegeneration. TSPO ligand-1 is involved in intracellular cholesterol transport and can be used as a biomarker for brain damage and neurodegeneration.

PROTAC Bcl-xL degrader-1 is a potent PROTAC composed of a Bcl-xL (Bcl-2 family member) ligand-binding group, a linker, and an IAP E3 ligases binding group, demonstrating effectiveness as a Bcl-xL degrader. It exhibits toxicity towards human platelets and MyLa 1929 cells, with IC50 values of 62 nM and 8.5 μM, respectively [1].

PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 ( IC 50 = 5 nM).

PROTAC BRD4 ligand-2 is a ligand for the target BRD4 protein used in the development of PROTAC CFT-2718.

PROTAC CRBN Degrader-1 is a chemical compound consisting of a cereblon (CRBN) ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group. It functions as a cereblon (CRBN) degrader[1].

PROTAC ERα Degrader-1 is a chemical compound. It consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group. This compound serves as a degrader of estrogen receptor-alpha (ERα).

FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].

PROTAC IRAK4 degrader-1 is a PROTAC (proteolysis-targeting chimera) compound that targets and degrades interleukin-1 receptor-associated kinase 4 (IRAK4).

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

PROTAC BRM degrader-1 (compound 17) serves as a PROTAC-based degrader targeting both BRM and BRG1, exhibiting DC50 values of 93 pM and 4.9 nM, respectively [1].

PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-targeting PROTAC small molecule that effectively induces apoptosis in MDA-MB-231 cells by mediating eEF2K degradation [1].

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, induces Bcr-Abl degradation via the ubiquitin-proteasome pathway and exhibits antiproliferative effects on K562 cells, indicating its potential in cancer research [1].

PROTAC KRAS G12C degrader-1, a cereblon-based degrader, promotes CRBN/KRAS G12C dimerization and facilitates the degradation of GFP-KRAS G12C in reporter cells [1].

DENV Ligand 1 serves as a ligand for the DENV E protein. It is utilized in the synthesis of the PROTAC degrader ZXH-8-004.

PROTAC tubulin-Degrader-1 (Compound W13) functions as an inhibitor of PROTAC tubulin and exhibits anti-tumor activity against human lung cancer.

PROTAC CBP P300 Degrader-1 is an effective compound that potently degrades CBP P300, significantly reducing cell viability in various cancer cell lines.

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces NSD3 degradation in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, arrests the cell cycle, and diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

PROTAC GDI2 Degrader-1 (Compound 21) is a potent degrader of PROTAC GDI2, demonstrating outstanding antitumor activity in vivo within pancreatic xenograft models that overexpress GDI2 [1].

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

Compound A6, a potent and selective PROTAC HDAC6 degrader, exhibits a DC50 of 3.5 nM. It demonstrates notable antiproliferative activity by inducing apoptosis in myeloid leukemia cell lines [1].