protac

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

PROTAC BRD4 Degrader-5 is a PROTAC that efficiently degrades BRD4 in HER2-positive and -negative breast cancer cell lines, and is formed by linking von Hippel-Lindau ligand to BRD4 ligand.

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.

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

CCT367766 is a potent, PROTAC-based, third-generation, iso-functional pirin-targeted protein degradation probe (PDP) that depletes pirin expression at low concentrations.CCT367766 has an IC50 value of 490 nM for the CRBN-DDB1 complex.CCT367766 has a good affinity for recombinant pirin and CRBN. CCT367766 has a good affinity for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. cct367766 is a potent orally active protein that reduces the expression of pirin at low concentrations.

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.

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.

Br-C10-methyl ester, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in the synthesis of a series of PROTACs (MS432). This compound incorporates a dual-ligand system connected via a linker; notably, one ligand interacts with the VHL portion.

Monoethyl pimelate is a PROTAC linker, which refers to the alkyl ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader[1].