E3 Ligase Ligand-Linker Conjugates 22 incorporates an E3 ligase ligand and a linker, can be used for the treatment of EZH2-mediated cancer.

E3 ligase Ligand 3 is a ligand of E3 ligase, used in PROTAC technology.

dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.

ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).

TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells Apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research.

SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML).

SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL).

NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB).

PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces Apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.

ACBI2 is a highly potent and orally active VHL PROTAC (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.

MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.

PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research.

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs.

4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.

CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein.

MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research.

KTX-951 is a PROTAC targeting IRAK4 degradation (DC50=18 nM). KTX-951 (10 mg/kg) shows the oral bioavailability (F%) of 22% in a rat model. KTX-951 has good anticancer potential.

3-Mercaptopropanyl-N-hydroxysuccinimide ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

N3-PEG3-CH2CH2COOH a PEG-based PROTAC linker can be used in the synthesis of BI-3663, BI-4216 and BI-0319. Azido-PEG3-acid is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1. PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM.

Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.

Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate which can be used for synthesizing dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.

VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266. ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.

Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852. UNC6852 is an EED-targeted bivalent chemical degrader.

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1. PROTAC B-Raf degrader 1 has anti-cancer activity.