Azido-PEG2-VHL is a multikinase degrader which can be used in the synthesis of PROTACs[1].
PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1[1].
HaloPROTAC 2, a chloroalkane-containing PROTAC, induces degradation of HaloTag fusion proteins.
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)[1].
BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].
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].
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].
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 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].
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].
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.
XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1[1].
The compound is a new angiogenesis inhibitor, which can be used to normalize abnormal blood vessels and effectively deliver drugs.
YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression[1].
TL12-186 is a CRBN-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM)[1].
dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1[1].
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[1].
XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1)[1].
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader[1].
MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool (PROTAC) for exploring the PRMT5 functions in health and disease.
dBET23 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=50 nM) in cellular degradation assays.
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer[1].
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1].
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells[1].
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[1].
SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization[1].
dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].