(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to VHL and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).

KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.

Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker.

NH2-PEG5-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH2-PEG5-OH is also a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.

THP-PEG6-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. THP-PEG6-OH is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker.

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.

SNIPER(ABL)-062 is a novel, potent SNIPER molecule that tethers BCR-ABL inhibitor to a ligand of IAP, causes potent BCR-ABL degradation.

QCA570 is a novel, highly potent efficacious BET degrader (PROTAC).

HDAC6 degrader 9c (dHDAC6 9c) is a bifunctional molecule (dHDAC6) that could selectively degrade HDAC6, by conjugating non-selective HDAC inhibitor to a thalidomide-type E3 ligase ligand.

E3 Ligand-Linker Conjugate 5 is an E3 ligase ligand-linker conjugate for PROTAC..

BTK PROTAC 9 is a novel potent PROTAC for BTK with DC50 of 5.9 nM in cultured Ramos cells, requires simultaneous engagement of BTK and CRBN to effectively degrade BTK.

BTK PROTAC 10 is a novel potent PROTAC for BTK with DC50 of 1.1 nM in cultured Ramos cells.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligand- Linker Conjugate for PROTAC..

A VHL ligand for PROTAC..

A VHL ligand for PROTAC..

A PEG4 linker for PROTAC..

A PEG3 linker for PROTAC..

A PEG2 linker for PROTAC..

A PEG linker for PROTAC..

A PEG linker for PROTAC..

A PEG linker for PROTAC..

A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM)..

A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε.