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PROTACPROTACs
PROteolysis TArgeting Chimeras (PROTACs) achieve degradation through "hijacking" the cell's ubiquitin–proteasome system (UPS) by bringing together the target protein and an E3 ligase. Because PROTACs need only to bind their targets with high selectivity (rather than inhibit the target protein's enzymatic activity), there are currently many efforts to retool previously ineffective inhibitor molecules as PROTACs for next-generation drugs.
AU-15330
T399542380274-50-8In house
AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]
- $139
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ARV-471
T397102229711-68-4In house
Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.
- $186
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c004019
T678342417159-57-8In house
C004019 is a small molecule PROTAC capable of targeting tau for selective protein degradation from the cell, while recruiting tau and E3 ligase (Vhl) for selective enhancement of tau ubiquitination and proteollyzation. C004019 is a candidate for AD and related tau protein diseases.
- $263
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luxdegalutamide
T751292750830-09-0
Luxdegalutamide (ARV-766) is a novel, potent, and orally bioavailable proteolytic targeting chimera (PROTAC) protein degrader that degrades not only wild-type AR but also clinically relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations.
- $318
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NX-5948
T751242649400-34-8
NX-5948 (BTK-IN-24) is an orally bioavailable and blood-brain barrier-penetrable PROTAC BTK degrader with anti-inflammatory and antitumor activities. It induces BTK protein degradation via the cereblon E3 ligase complex, inhibiting B cell activation.
- $378
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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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xStAx-VHLL TFA
T36275L
xStAx-VHLL TFA is a β-catenin degrader formed by coupling xStAx to VHL ligand, has anti-cancer activity, inhibits Wnt signaling, and can be used in the study of cancer.
- $94
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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.
- $510
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TCO-PEG4-NHS ester
T170171613439-69-2
TCO-PEG4-NHS ester is a PROTAC linker bridge in the PEG class, used for synthesizing various PROTAC molecules. As a cleavable and synthetic ADC, it is also utilized in the synthesis of antibody-drug conjugates (ADCs).
- $61
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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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ARD-2128
T396952222111-87-5
ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) that degrades the androgen receptor (AR), effectively reducing AR protein levels, suppressing AR-regulated gene expression in tumor tissues, and inhibiting tumor growth without evident toxicity. This compound holds promise for prostate cancer research.
- $228
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dBET6
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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XY028-140
T366942229974-83-6
XY028-140 is a selective CDK4 CDK6 degrade and inhibits both CDK4 6 expression and activity in cancer cells. XY028-140 is a PROTAC connected by ligands for Cereblon and CDK.
- $34
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KT-474
T744112432994-31-3
KT-474 (KYM-001) is a PROTAC degrader targeting interleukin-1 receptor-associated kinase 4 (IRAK4) with antitumor activity for the study of autoimmune, inflammatory, and cardiovascular disease disorders.
- $247
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(Iso)-MS4322
T402332601727-80-2In house
(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.
- $489
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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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ARV-393
T843162851885-95-3
ARV-393 is a PROTAC degrader targeting BCL6 with the advantage of being highly potent and orally available.ARV-393 recruits BCL6 and E3 ligase cerebellum to rapidly degrade BCL6 through the cell's natural ubiquitin proteasome system for the treatment of diffuse large b-cell lymphoma (DLBCL) and non-Hodgkin's lymphoma (NHL).
- $223
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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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protac braf-v600e degrader-1
T87452417296-84-3
PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.
- $115
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dCBP-1
T93702484739-25-3
dCBP-1 is a chemical degrader of p300 CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300 CBP. Degradation of p300 CBP by dCBP-1 leads to effective multiple myeloma cell killing.
- $96
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Benzyl-PEG12-alcohol
T396892218463-17-1
Benzyl-PEG12-alcohol is a PEG-based linker for PROTACs, connecting two essential ligands to form PROTAC molecules. This linker facilitates selective protein degradation by utilizing the ubiquitin-proteasome system within cells.
- $50
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YD23
T779732951015-29-3
YD23 is a PROTAC that induces SMARCA2 degradation, has anticancer activity, and selectively inhibits the growth of SMARCA4 mutant lung cancer cells in vitro.
- $81
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YX-2-107
T747102417408-46-7
YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).
- $226
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FKBP12 PROTAC RC32
T136942375555-66-9
FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.
- $215
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