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PROTACPROTAC Selection
Selection of target proteins for PROTAC can be based on the following considerations: 1. Whether the protein is specific or not, non-specific proteins can cause off-target toxicity; 2. Whether the protein belongs to the molecules that can be degraded by PROTAC, and it has been reported that the targets that can be used for PROTAC include, kinases (MEK, KRAS, CDK, and Bcr/Abl), transcription factors (e.g. p53, STAT, RAR, ER, and AR), epigenetic factors (e.g., HDAC and BET bromodomain), and E3 ligases themselves (e.g., MDM2), among others; 3. Whether or not the protein has been reported to have a ligand or crystalline form that can be commercially engineered.
AK-1690
T2010322984505-88-4
AK-1690 is a potent and selective STAT6 PROTAC degrader that induces degradation of STAT6 proteins in cells (DC50=1 nM) and depletes STAT6 proteins in mouse tissues, which can be used in cancer research.
- $297
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MT-802
T161572231744-29-7
MT-802 is an effective BTK degrader based on PROTAC technology (DC50: 1 nM). MT-802 has the potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
- $88
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THAL-SNS-032
T170692139287-33-3
THAL-SNS-032 is a PROTAC designed to selectively degrade CDK9.
- $118
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ACBI1
T173502375564-55-7
ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.
- $98
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JQAD1
T411802417097-18-6
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.
- $131
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BSJ-03-123
T53952361493-16-3
BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.
- $84
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MD-224
T119802136247-12-4
MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
- $64
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GSK215
T678432743427-26-9
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.
- $127
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ZXH-1-161
T630102407654-51-5
ZXH-1-161 is a potent Cereblon (CRBN) modulator PROTAC that selectively degrades GSPT1 for use in multiple myeloma research.
- $1,490
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JB170
T741742705844-82-0
JB170 is a highly efficient and specific Aurora A degradator (DC50 = 28 nM). The PROTAC is composed of Alisertib and Thalidomide, with an EC50 value for AURORA-A that is ten times that of AURORA-B. It induces S-phase arrest in cell growth and inhibits the non-catalytic function of the AURORA-A kinase.
- $100
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T885942879251-63-3
dWIZ-1 ((rac)-dWIZ-1) is a potent WIZ molecular gel degrader that recruits WIZ (ZF7) to the cereblon thereby inducing degradation and thus induction of haemoglobin fetalis (HbF) in erythroblasts, which can be used to study sickle cell disease (SCD).
- $195
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TD-165
T187872305936-56-3
TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1].
- $105
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Homo-PROTAC pVHL30 degrader 1
T137222244684-49-7
Homo-PROTAC pVHL30 degrader 1 is a potent PROTAC-based degrader of pVHL30.
- $30
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dCeMM1
T67778118719-16-7
dCeMM1, a RBM39 glue degrader, re-directs the activity of the CRL4DCAF15 ligase and decreases RBM39 expression levels in WT KBM7 cells.
- $30
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Homo-PROTAC cereblon degrader 1
T137212244520-98-5
Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
- $74
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A1874
T54422064292-12-0
A1874 is a nutlin-based and BRD4-degrading PROTAC which induces BRD4 degradation in cells. Effective in inhibiting many cancer cell lines proliferation.
- $84
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SD-436
T2033952497585-50-7
SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models.
- $993
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AT6
T135612098836-50-9
AT6 is a PROTAC AT1 analog which is a highly selective bromodomain (Brd4) degrader.
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PROTAC BRD9 Degrader-1
T125602097971-01-0
PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.
- $733
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MS432
T13782
MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
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dFKBP-1
T185971799711-22-0
dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].
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PROTAC MDM2 Degrader-2
T186322249944-99-6
PROTAC MDM2 Degrader-2, designed using PROTAC technology, functions as a MDM2 degrader. It consists of a highly potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase, facilitating the degradation of MDM2[1].
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PROTAC ERRα Degrader-2
T186092306388-85-0
PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].
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CP-10
T136272366268-80-4
CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.
- $728
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