Epigenetic Reader Domain Ligand

PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.

Nrf2 activator-1 is an Nrf2 activator that acts on the Keap1-Nrf2 pathway. Nrf2 activation enhances antioxidant response-related transcription and promotes downstream cytoprotective responses such as NQO1. Nrf2 activator-1 is used in research on Nrf2 signaling and oxidative stress.

Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC₅₀ of 10 nM, and with a K_i of 2.3 nM. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

BRD9 ligand-11 is a BRD9 PROTAC ligand. BRD9 ligand-11 can be conjugated with E3 ligase Ligand (HY-125845) and linker to synthesize PROTAC BRD9 Degrader-11 (HY-181951). PROTAC BRD9 Degrader-11 can be used for cancer research.

BRD4/FKBP12 ligand 2 is a heterobifunctional BRD4 and FKBP12 (K_d of 1.0 nM) ligand. BRD4/FKBP12 ligand 2 has positive cooperativity in BRD4 binding when pre-bound to FKBP12, and FKBP12-dependent cytotoxicity in cancer cells via the CellTrap effect. BRD4/FKBP12 ligand 2 can be used for the research of hematopoietic malignancy, multiple myeloma, prostate carcinoma, acute myeloid leukemia.

PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37 (HY-175225).

BRD3/BRD4-L ligand-2 is a BRD3/BRD4-L ligand. BRD3/BRD4-L ligand-2 serves as a ligand for the target protein in the design and development of PROTAC BRD3/BRD4-L degraders, such as PROTAC BRD3/BRD4-L degrader-2 (HY-149948). BRD3/BRD4-L ligand-2 can be used in cancer research.

BRD9 ligand-14 is a BRD9 ligand that acts as a protein-of-interest ligand for synthesis of BRD9 PROTAC degraders. BRD9 ligand-14 can be used for research in acute myeloid leukemia.

BRD3 ligand-1 is a BRD3 ligand that can be used in studies related to PROTAC synthesis, such as serving as the target protein ligand for PROTAC BRD3 degrader-1 (HY-180889).

QS-57 is a heterobifunctional targeted protein localization (TPL) agent. QS-57 binds to BRD4 via its JQ1 domain and covalently targets 14-3-3σ to form a ternary complex. QS-57 sequesters nuclear BRD4 in the cytoplasm, impairing the nuclear transcriptional regulatory function mediated by BRD4. QS-57 significantly reduces the nuclear BRD4 protein level and increases the cytoplasmic BRD4 protein abundance in cancer cells. QS-57 can be used for research on breast cancer and colorectal cancer.

AR/BET ligand-1 is a AR/BET ligand, which can be used for the synthesis of PROTACs, such as PROTAC AR/BET protein degrader-1 (HY-160262).

PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker. PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu can be used for synthesis of PROTAC BRD4 Degrader-14 (HY-138637).

CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers.

BRD4 ligand 16 is a BRD4 ligand. BRD4 ligand 16 can serve as a ligand for the target protein in the synthesis of BRD4 PROTAC degraders, such as PROTAC BRD4 Degrader-17 (HY-143328). BRD4 ligand 16 is suitable for use in cancer research.

TAF1 ligand 1 is a TAF1 ligand. TAF1 ligand 1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as ZS3-046 (HY-176457).

BRD4/FKBP12 ligand 1 is a heterobifunctional BRD4 and FKBP12 (K_d of 0.4 nM) ligand. BRD4/FKBP12 ligand 1 has positive cooperativity in BRD4 binding when pre-bound to FKBP12, and FKBP12-dependent cytotoxicity in cancer cells via the CellTrap effect. BRD4/FKBP12 ligand 1 can be used for the research of acute myeloid leukemia, multiple myeloma, prostate carcinoma.

BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1 (HY-175678).

FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1(HY-175610).

BRD4 ligand 15 (compound 5) is a BRD4 ligand and alkyne-modified chalcone derivative, which serves as a building block for the synthesis of BRD4-targeting PROTAC TKP-5 (HY-182370).

BRD9 ligand-3 is a BRD9 ligand. BRD9 ligand-3 serves as a PROTAC target protein ligand for the synthesis of PROTACs, such as PROTAC BRD9 Degrader-4 (HY-145403). BRD9 ligand-3 is applicable to cancer-related research.