PROTAC

MS4322 (YS43-22) is a first-in-class PRMT5 degrader and a valuable chemical tool (PROTAC) for exploring the PRMT5 functions in health and disease.

BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.

VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.

PROTAC PARP1 degrader is a bifunctional small molecule composed of a PARP1-binding ligand covalently linked via a linker to an E3 ubiquitin ligase ligand, which can potently induce PARP1 cleavage and programmed cell death.

MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37?nM for binding affinity to ALK.

ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.

THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 linked to Pomalidomide with a linker. Anti-cancer activity.

MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively.

JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.

PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.

PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a potent and selective PRMT5 (protein arginine methyltransferase 5) degrader, and inhibits growth of multiple cancer cell lines.

SB1-G-187, a PROTAC, is a multi-kinase degrader.

DB-0646, a PROTAC, is a multi-kinase degrader.