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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.
Fmoc-PEA
T17977329223-23-6In house
Fmoc-PEA (Example 1-2) is utilized as a cleavable linker for antibody-drug conjugates (ADC).
- $38
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ARV-825
T54341818885-28-7
ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.
- $60
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Nrf2 degrader 30
T2013953025286-29-4
Nrf2 degrader 30 is a small molecule PROTAC that inhibits the degradation of Nrf2, thereby enhancing its activity. Nrf2 is a key transcription factor that regulates cellular antioxidant responses and various protective mechanisms. The activity of Nrf2 is primarily regulated by its interaction with Keap1, which serves as an E3 ubiquitin ligase complex adapter to promote Nrf2 ubiquitination and proteasomal degradation。
- $795
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A947
T746862378056-80-3
A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells.
- $1,070
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cis VH 032, amine dihydrochloride
T354782376990-32-6
cis VH 032, amine dihydrochloride ((S,S,S)-AHPC) is a negative control for the functionalized VHL ligand VH 032, amine .
- $31
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dBET6
Cited
T51301950634-92-0
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
- $48
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CitedMT-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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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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Dbet57
T54401883863-52-2
dBET57 is heterobifunctional degrader of BRD4 based on the PROTAC technology, exhibits significant degradation of BRD4BD1 with a DC50 5h of 500 nM ,and inactive on BRD4BD2
- $42
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ARV-771 Cited
T54351949837-12-0
ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.
- $55
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CitedBSJ-03-123
T53952361493-16-3
BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.
- $84
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PROTAC CDK9 degrader 4
T399962411021-01-5
PROTAC CDK9 degrader 4 is a highly potent CDK9 degrader that targets transcriptional regulation and has potential anticancer activity for the study of acute myelogenous leukemia (AML).
- $322
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dBRD9 HCl
T31221L2341840-98-8
dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.
- $197
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JQAD1 Cited
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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CitedARV-393
T843162851885-95-3
ARV-393 is a BCL6 PROTAC degrader with DC50 and GI50 values of <1 nM in both DLBCL and BL cell lines. ARV-393 inhibits tumor volume in multiple tumor xenograft models.
- $223
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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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BETd-260
T145502093388-62-4In house
BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.
- $132
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β-NF-JQ1
T105262380000-55-3In house
β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.
- $97
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MS4078
T161532229036-62-6
MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.
- $44
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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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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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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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VH032
T291061448188-62-2In house
VH032 commonly used as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component.VH032 is a VHL HIF-1α interaction inhibitor with a KdPROTACs, which can recruit von Hippel-Lindau (VHL) proteins as a ligand of VHL.
- $44
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UNC6852
T139542688842-08-0
UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
- $135
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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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dBET1
T44951799711-21-9
dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis.
- $48
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Gefitinib-based PROTAC 3
T54372230821-27-7
Gefitinib-based PROTAC 3, which connects an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively[1].
- $38
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dCeMM2
T61477296771-07-8
dCeMM2 is a glue degrader. dCeMM2 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, leading to the ubiquitination and degradation of cyclin K.
- $31
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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.
- $32
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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.
- $228
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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.
- $228
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DT2216
T136652365172-42-3
DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hipp
- $71
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FKBP12 PROTAC dTAG-13
T112912064175-41-1
FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.
- TBD
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FKBP12 PROTAC dTAG-7
T112922064175-32-0In house
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
- TBD
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dMCL1-2
T136572351218-88-5In house
dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.
- $8,005
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QCA570
T167012207569-08-0In house
QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).
- Inquiry Price
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Halo PROTAC 1
T179952241668-45-9
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].
- Inquiry Price
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PROTAC FLT-3 degrader 1
T125552230826-81-8
PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.
- Inquiry Price
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BETd-246
T145492140289-17-2
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
- $539
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KB02-JQ1
T180602384184-44-3
KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].
- Inquiry Price
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PROTAC EED degrader-2
T12554
PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.
- Inquiry Price
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PROTAC BET Degrader-1
T138492093386-22-0
PROTAC BET Degrader-1 is a potent BET degrader utilizing the PROTAC mechanism.
- $456
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VH032-PEG5-C6-Cl
T179961799506-06-1
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule that includes the VH032-based VHL ligand and a 5-unit PEG linker, capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
- Inquiry Price
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TD-428
T13105
TD-428 is a highly specific degrader of BRD4(DC50 of 0.32 nM). TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
- Inquiry Price
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PROTAC B-Raf degrader 1
T125562364367-27-9
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.
- $431
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PROTAC BRD4 Degrader-1
T138332133360-00-4
PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).
- Inquiry Price
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