Mcl1-IN-14 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. Mcl1-IN-14 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity[1].
PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines[1].
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation[1].
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research[1].
PROTAC VEGFR-2 degrader-2（PROTAC-4）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM)[1].
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1].
PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
PROTAC AR-V7 degrader-2 is an AR-based PROTAC. PROTAC AR-V7 degrader-2 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. PROTAC AR-V7 degrader-2 induces apoptosis[1].
A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε; a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.
PROTAC EGFR degrader 6 (Compound 2), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an E3 ubiquitin ligase (Pomalidomide; HY-10984)[1].
HJM-561 is a potent, selective, orally bioavailable EGFR PROTAC. HJM-561 overcomes osimertinib (HY-15772)-resistant EGFR triple mutations and has anti-tumor activity[1].
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively[1].
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader[1].
PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC BRD4 degrader[1].
FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells; causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras, and an unexpected superior antiproliferative effect of pan-BET bromodomain degradation over selective BRD4 degradation, characterize immediate effects of KRASG12V loss on proteomic signaling, and demonstrate rapid degradation in vivo.
dBET57 is a potent and selective heterobifunctional degrader of BRD4 based on the PROTAC technology, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2[1].
PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation[1].
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer[1].
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[1].
RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
dBRD9 is a PROTAC that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex; exhibits markedly enhanced potency compared to parental ligands (10-100 fold).
DB0614 (Example 21) is a bifunctional compound targeted protein degradation of kinases. DB0614 degrades AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
PROTAC ER Degrader-4 is a PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM[1].
XF056-132 is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader[1].
PROTAC BRD4 Degrader-15 is a potent BRD4 degrader, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC50 values of 19 ± 6 nM and 56 ± 12 nM, respectively[1].
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[1].
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research[1].