- Cat. No.
- A19547
dTRIM24
dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
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PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.
dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader.
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader.
PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
PROTAC CRABP-II Degrader-3 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase.
PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK.
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK.
DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology.
GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance.
Synonyms: SN-11; PROTAC cIAP1 degrader-4
SNIPER(CRABP)-11, also known as PROTAC cIAP1 degrader-4, is a potent protein degrader.
AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components.
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research.
dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies.
Synonyms: ARV-110
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer.
MS1943 is an orally active, PROTAC-based selective degrader of EZH2 that effectively reduces cellular EZH2 levels. It exhibits strong anticancer activity, showing cytotoxic effects in various triple-negative breast cancer (TNBC) cell lines while sparing normal cells. MS1943 maintains high potency in inhibiting EZH2 methyltransferase activity (IC₅₀ = 120 nM) and demonstrates high selectivity for EZH2, making it a promising candidate for epigenetic and cancer research.
MS177 is a fast-acting and effective PROTAC degrader targeting EZH2. It comprises a cereblon (CRBN) ligand, a linker, and the potent EZH2 enzymatic inhibitor C24 (IC₅₀: 12 nM). MS177 efficiently depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell proliferation, induction of apoptosis, and cell cycle arrest. It is a valuable tool for epigenetic and cancer research.
Synonyms: ARV471
Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation.
TL12-186 is a cereblon-dependent PROTAC degrader with broad-spectrum activity against multiple kinases, including CDKs, BTK, FLT3, Aurora kinases, TEC, ULK, and ITK. It inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC₅₀ values of 73 nM and 55 nM, respectively, making it a valuable tool for studying kinase-driven signaling pathways and cancer biology.