Epigenetic Reader Domain Degrader

YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1^C1113A mutation.

PROTAC BRD4 Degrader-18 is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-18 binds to BRD4 and recruits E3 ubiquitin ligase, inducing ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-18 exhibits antiproliferative activity against ovarian cancer cell lines. PROTAC BRD4 Degrader-18 can be used in research related to ovarian cancer.

PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC₅₀ value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research.

PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC₅₀=0.09 nM) and BRD4 (IC₅₀=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia.

PROTAC BRD4 Degrader-16 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-16 induces sustained degradation of both long and short isoforms of BRD4 in cancer cells, causes cell cycle arrest, and exhibits only extremely low apoptosis effects. PROTAC BRD4 Degrader-16 can be used in studies related to acute myeloid leukemia.

MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC₅₀ of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells.

(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC₅₀ value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC₅₀ value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study.

PROTAC BRD4 Degrader-23 is a visible light-regulated BRD4 PROTAC degrader, with DC₅₀ values of 6871 nM and < 30 nM in the dark and under light exposure, respectively; its IC₅₀ values are 1172 nM and 140 nM under the corresponding conditions. PROTAC BRD4 Degrader-23 shows inhibited activity in dark environments, and recovers BRD4 degradation ability upon irradiation with 405 nm visible light. PROTAC BRD4 Degrader-23 inhibits tumor cell proliferation in a visible light-dependent manner. PROTAC BRD4 Degrader-23 can be used in studies of BRD4-dependent B-cell lymphoma.

PROTAC BRD4 Degrader-28 is a PROTAC degrader targeting BRD4, with a DC₅₀ of 5.4 nM for BRD4 in HEK293 cells. PROTAC BRD4 Degrader-28 binds to the CRBN E3 ubiquitin ligase, forms a ternary complex with BRD4, and thereby mediates the ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-28 can be used in cancer research.

PROTAC BRD4 Degrader-27 is a selective cereblon-mediated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-27 exhibits anticancer activity, induces G1 phase arrest, and inhibits DNA synthesis and colony formation. PROTAC BRD4 Degrader-27 suppresses HCC1806 tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-27 can be used in breast cancer-related research.

dBAZ2B is a BAZ2B PROTAC degrader, with a DC₅₀ of 19 nM. (Pink: BAZ2A/B ligand (HY-168449); Black: linker (HY-168450); Blue: VHL Ligand (HY-125905))

LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.

PROTAC BRD4 Degrader-50 is a BRD4 PROTAC degrader with a DC₅₀ of 11.4 nM (HEK293). PROTAC BRD4 Degrader-50 induces BRD4 degradation via the proteasome and CRBN. PROTAC BRD4 Degrader-50 is applicable to cancer research.

BRD4 degrader-4 (Compound 1-f) is a BRD4 degrader. BRD4 degrader-4 can be used for the research of cancer and other bromodomain related diseases.

SRG-II-19F (dCym-JQ1) is a BRDTBD1 PROTAC degrader. Its dCym moiety at one end binds to the N-terminal domain of ClpC1 (ClpC1NTD), while its JQ1 moiety at the other end binds to bromodomain 1 of BRDT (BRDTBD1). This molecule induces the degradation of BRDTBD1 by recruiting the BRDTBD1 substrate to the ClpC1P1P2 protease complex. SRG-II-19F serves as a research tool for studies related to mycobacterial protein degradation.

PROTAC BRD4 Degrader-47 is a heterobifunctional PROTAC that selectively degrades BRD4 in a SYVN1-dependent manner, with a DC₅₀ of 0.93 μM. PROTAC BRD4 Degrader-47 can be used in cancer-related research such as breast cancer.

MM-02-08 is a BRD4 PROTAC degrader with a DC₅₀ of approximately 10 nM. MM-02-08 mediates mono-ubiquitination and poly-ubiquitination modifications of target proteins without impairing cell viability. MM-02-08 is applicable to related research on triple-negative breast cancer, prostate cancer, and other diseases.

PROTAC BRD2 BD1 Degrader-1 is a potent and selective BRD2 BD1 PROTAC degrader, with a DC₅₀ of 65 nM, an EC₅₀ of 423 nM, and a K_d of 69 nM against BRD2 BD1. PROTAC BRD2 BD1 Degrader-1 induces the formation of a ternary complex between the BET bromodomain and the VHL E3 ubiquitin ligase complex, triggering VCB-dependent degradation of the target bromodomain. PROTAC BRD2 BD1 Degrader-1 can be used in cancer research.

PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC₅₀ of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia.

JV8 is a BRD4 PROTAC degrader with a target K_d of 0.65 μM. JV8 preferentially induces BRD4 degradation in the cytoplasm via the ubiquitin-proteasome system. JV8 exhibits dose-dependent and time-dependent BRD4 degradation activity and is capable of inducing cell apoptosis. JV8 inhibits tumor growth in a dose-dependent manner and induces BRD4 degradation in tumor tissues in vivo. JV8 can be used in research related to various cancers such as breast cancer and pancreatic cancer.