Benzyl-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

MS 177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

Benzyl-PEG1-propanol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Benzyl-PEG5-NHBoc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

A heterobifunctional small molecule PROTAC capable of cereblon mediated proteasomal degradation of CDK9.

CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.

TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.

Homo-PROTAC cereblon degrader 1, is a cereblon degrader.

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.

BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression.

PROTAC BTK Degrader-11 is a PROTAC degrader that can break down BTK, with a DC50 of 1.7 nM.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.

MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).

MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.

UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).

XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1.

Aurora kinase ligand-1 (Compound I-4) is an Aurora kinase B (AURKB) PROTAC ligand. Aurora kinase ligand-1 can be conjugated with E3 ligase Ligand and linker to synthesize AURKB PROTAC degrader MS44. MS44 can be used for cancer research.

IRAK4 ligand-14 is a ligand for IRAK4. IRAK4 ligand-14 can be used for synthesizing PROTACs such as APH02174.

SMARCA2/4-ligand-6 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-ligand-6 can be used for the synthesis of SMARCA2/4-ligand-6.

PDE4 ligand 2 is a CRBN E3 ligase ligand. PDE4 ligand 2 can be used to synthesize PROTAC such as PDE4 degrader-1. PDE4 ligand 2 can be studied in research for autoimmune and anti-inflammatory diseases.

KRASG12C ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC YN14-H. YN14-H is a PROTAC degrader targeting KRASG12C and has antitumor activity.

Oxide-DFHBI-demethyl is a target aptamer ligand (Ligand for Target Protein for PROTAC). Oxide-DFHBI-demethyl can be used for synthesis of RNA aptamer-based PROTAC Dth.

DOT1L ligand-1 is a DOT1L ligand. DOT1L ligand-1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as MS2133.

PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37.