Epigenetic Reader Domain Degrader

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (K_d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.

PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC₅₀ values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)).\n

dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 selectively binds to BRD4 BD1 to form a BRD4-dHTC3 complex, which cooperatively recruits the SCF^FBXO3 E3 ubiquitin ligase and mediates the degradation of BRD4 via the ubiquitin-proteasome pathway. dHTC3 induces proteasome- and CRL-dependent BRD4 degradation with no hook effect. dHTC3 can be used in related research on acute myeloid leukemia.

EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.

TrimTAC1 is a TRIM21-based PROTAC degrader targeting BRD4, with a DC₅₀ of 0.649 nM. TrimTAC1 selectively degrades multimeric proteins, including those localized in biomolecular condensates, while exerting no effect on monomeric proteins in the dilute phase. This degradation effect can be blocked by Bortezomib (HY-10227) or TAK-243 (HY-100487). TrimTAC1 can be used in research related to pancreatic cancer and autoimmune diseases.

MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells.

dBRD9 dihydrochloride is a BRD9 PROTAC degrader. dBRD9 dihydrochloride reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 dihydrochloride can be used in research related to acute myeloid leukemia.

CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer.

L134 is a BRD4 PROTAC degrader with a DC₅₀ of 7.36 nM. L134 induces BRD4 protein degradation without inhibiting BRD4 gene expression, and recruits the E3 ubiquitin ligase DCAF11 to mediate this process, which can be blocked by proteasome inhibitors (MG132 (HY-13259), PS341 (HY-10227)) and E1 ubiquitin ligase inhibitors (PYR41 (HY-13296), MLN4924 (HY-70062)). L134 inhibits cancer cell migration, promotes cancer cell apoptosis and exerts antiproliferative activity. L134 can be used in studies related to triple-negative breast cancer.

AMX-883 a selective and orally active BRD9 molecular glue degrader that drives differentiation in acute myeloid leukaemia. AMX-883 shows selectivity over all other bromodomain containing proteins and proteome wide. AMX-883 does not employ the commonly used E3 ligases (cereblon, VHL) but instead drives degradation via DCAF16 as a targeted glue. AMX-883 can be used for the study of acute myeloid leukaemia (AML).

PROTAC BRD4 Degrader linker conjugate-2 is a PROTAC-based BRD4 degrader.

PROTAC BRD9 Degrader-5 is a BRD9 PROTAC degrader. PROTAC BRD9 Degrader-5 is used in research on acute myeloid leukemia, rhabdoid tumor, synovial sarcoma, and multiple myeloma.

PROTAC BRD4 Degrader-45 is a PROTAC degrader targeting BRD4, with a DC₅₀ of 43 nM. PROTAC BRD4 Degrader-45 is applicable to studies on membrane-permeable PROTACs.

XYD224 is a selective BRD9 PROTAC degrader with a DC₅₀ of 7.3 nM. XYD224 inhibits the proliferation of acute myeloid leukemia cells. XYD224 suppresses tumor growth in xenograft models. XYD224 is applicable for the research of acute myeloid leukemia (AML).

JQ1-S (GlcNAc) Cq is a sugar-modified BRD4 PROTAC degrader with a DC₅₀ of 2.1 μM. JQ1-S (GlcNAc) Cq inhibits the formation of the ternary complex between CRBN and BRD4 (BD1/BD2). JQ1-S (GlcNAc) Cq serves as a substrate for O-GlcNAcase, which cleaves its O-GlcNAc domain to restore binding ability with CRBN, thereby forming a BRD4-containing ternary complex and triggering ubiquitination and proteasomal degradation of BRD4. JQ1-S (GlcNAc) Cq is applicable for cancer research.

PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader with a DC₅₀ of 0.649 nM. It has a K_d of 123 nM for TRIM21. PROTAC BRD4 Degrader-36 recruits the E3 ubiquitin ligase TRIM21 (K_d = 123 nM) to BRD4, leading to ubiquitination and subsequent degradation of BRD4. PROTAC BRD4 Degrader-36 exhibits cytotoxicity against PANC-1 cells (GI₅₀ = 0.103 μM). It can be used in research related to pancreatic cancer.

BRD9 Degrader-4 is a bifunctional targeted degrader of the BRD9 protein, which promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of the CRBN or VHL E3 ligases.

PROTAC BRD9 Degrader-6 (Compound D1) is a racemic PROTAC degrader that recruits cereblon to induce targeted degradation of BRD9. PROTAC BRD9 Degrader-6 has an IC₅₀ of 0.13 nM in SYO-1 cells. It can be used in research on BAF complex-related diseases, such as cancer, infections and synovial sarcoma.

PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC₅₀ of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs.