protac

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

C004019 is a small molecule PROTAC capable of targeting tau for selective protein degradation from the cell, while recruiting tau and E3 ligase (Vhl) for selective enhancement of tau ubiquitination and proteollyzation. C004019 is a candidate for AD and related tau protein diseases.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

KT-474 (KYM-001) is a PROTAC degrader targeting interleukin-1 receptor-associated kinase 4 (IRAK4) with antitumor activity for the study of autoimmune, inflammatory, and cardiovascular disease disorders.

Luxdegalutamide (ARV-766) is a novel, potent, and orally bioavailable proteolytic targeting chimera (PROTAC) protein degrader that degrades not only wild-type AR but also clinically relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.

ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.

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

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.

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.

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

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

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

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.

PROTAC BET-binding moiety 1 is a crucial intermediate used in synthesizing high-affinity BET inhibitors.

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

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

PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].

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

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 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 BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.