- Signaling Pathways
- PROTAC
- Ligands for Target Protein for PROTAC
Ligands for Target Protein for PROTAC
Target Protein-binding Moiety
The PROTAC molecule consists of a target protein ligand and an E3 ubiquitin ligase ligand, with a linker binds them together. The ligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.
Target proteins are usually proteins whose overexpression or accumulation may play important roles in the progress of diseases. Numbers of PROTACs have been developed to degrade kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), epigenetic tools (such as HDAC and BET bromodomain) and E3 ligase themselves (such as MDM2).
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Ligands for Target Protein for PROTAC Inhibitors
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Ligands for Target Protein for PROTAC Chemicals
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Ligands for Target Protein for PROTAC Degrader
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Ligands for Target Protein for PROTAC Controls
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Ligands for Target Protein for PROTAC Ligands
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Ligands for Target Protein for PROTAC Related Products (608)
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Related Compound Screening Libraries (1)
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Bortezomib
0 ImagesSynonyms: PS-341; LDP-341; NSC 681239Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs). -
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Dasatinib
0 ImagesSynonyms: BMS-354825Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier. -
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- (+)-JQ-1
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- Oleic acid
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Melatonin
0 ImagesMelatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress. -
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- (Z)-Sunitinib carboxylic acid
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HDAC4 ligand-2
0 ImagesCat. No.: HY-W039803CAS No.: 340736-76-7 -
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- SMARCA2/4-ligand-8
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- Ibrutinib
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Crizotinib
0 ImagesSynonyms: PF-02341066Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition. -
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iFSP1
0 ImagesiFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A). -
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Inobrodib
0 ImagesSynonyms: CCS1477Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. -
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Tranylcypromine hydrochloride
0 ImagesTranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression. -
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- JQ-1 carboxylic acid
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STING-IN-2
0 ImagesSTING-IN-2 (C-170) is a potent and covalent STING inhibitor. STING-IN-2 efficiently inhibits both mouse STING (mmSTING) and human STING (hsSTING). STING-IN-2 can be used for autoinflammatory disease research. -
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BI-7273
0 ImagesBI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. -
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- SI-109
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- SLF
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- CBP/p300 ligand 2
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- CCR7 Ligand 1
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