AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity[1].
CRBN-6-5-5-VHL is a potent and selective cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3[1].
BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1].
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[1].
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1].
ERK-CLIPTAC is a PROTAC molecule that triggers the degradation of ERK[1].
PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].
PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer[1].
CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].
ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER), with an DC50 of 0.17 nM in MCF-7 cells[1].
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].
Dovitinib RIBOTAC TFA is a targeted RNA degrader that cleaves pre-miR-21 with enhanced potency and selectivity.
PROTAC RIPK degrader-6 (example 1) is a PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder[1].
dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6)[1].
PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression[1].
CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.
E3 ligase Ligand 9 is a Ligand of BETd-260 for E3 Ligase used in PROTAC. BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 51 pM against BRD4 protein in RS4;11 leukemia cell line[1].
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader[1].
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44)[1].
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research[1].
PROTAC Her3 Degrader-8 (Compound PP2) is a PROTAC that can degrade Her3 protein in vitro and cell experiments, and can be used to study diseases regulated by HER family proteins[1].
PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research[1].
dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.
SNX7886 is a potent protac degrader of CDK8/19. SNX7886 degrades CDK 8 and CDK 19 with 90% and 80% degradation in 293 cells, respectively[1].
XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1[1].
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].