Epigenetic Reader Domain Degrader

Epigenetic Reader Domain Degraders (80):

Cat. No.	Product Name	Effect	Purity

HY-158764

PROTAC BET Degrader-12	Degrader	98.10%
PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC₅₀ of 305.2 nM. (Pink: ligand for target protein (+)-JQ-1 (HY-13030); Black: linker (HY-159077); Blue: ligand for E3 ligase (HY-159076))

HY-161779

PLX-3618	Degrader
PLX-3618 is a molecular glue, that degrades BRD4 with DC₅₀ of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models.

HY-163410

AU-24118	Degrader	99.10%
AU-24118 is orally bioavailable proteolysis targeting chimera (PROTAC) degrader of mSWI/SNF ATPases (SMARCA2 and SMARCA4) and PBRM1.

HY-117690

dBRD9	Degrader	99.89%
dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.

HY-153385

TMX1	Degrader	99.09%
TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to the BRD4BD2, leading to BRD4 degradation.

HY-156828

MMH2	Degrader	98.03%
MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2).

HY-156568B

SMD-3040 formate	Degrader	99.90%
SMD-3040 formate is a potent and selective smarca2 protac degrader with strong in vivo antitumor activity.

HY-101460

Tz-Thalidomide	Degrader	98.01%
Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC₅₀s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

HY-153459

PROTAC BRD4 Degrader-19	Degrader	98.83%
PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. PROTAC BRD4 Degrader-19 can be used in cancer research.

HY-156827

MMH1	Degrader	98.08%
MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4_BD2).

HY-139707

Thalidomide-NH-CBP/p300 ligand 2	Degrader	98.55%
Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440).

HY-156568A

SMD-3040 TFA	Degrader	99.90%
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models.

HY-149878

BD-9136	Degrader	98.81%
BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity.(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))

HY-136857

BRD4 degrader-3	Degrader
BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC₅₀s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-156568

SMD-3040	Degrader	99.91%
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC₅₀: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models.

HY-107425A

cis-MZ 1	Degrader
cis-MZ 1 is a negative control of MZ 1 (HY-107425). cis-MZ 1 is a PROTAC.html" class="link-product" target="_blank">PROTAC targeting to BRD4.

HY-138636

PROTAC BRD4 Degrader-13	Degrader
PROTAC BRD4 Degrader-13 (compound 9d) is a von Hippel-Lindau system-based PROTAC BRD4 degrader with a linker that can be coupled to ADC antibodies to form PACs (PROTAC-antibody Conjugates). PROTAC BRD4 Degrader-13 can be coupled to STEAP1 and CLL1 antibodies to degrade BRD4 protein in PC3 prostate cancer cells with DC₅₀ values of 0.025 nM and 6.0 nM, respectively.

HY-161346

EBET-1055	Degrader
EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. 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.

HY-156744

DBr-1	Degrader
DBr-1 is a potent BRD9 PROTAC degrader (K_D: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352).

HY-153632

PROTAC BRD9 Degrader-6	Degrader	98.19%
PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC₅₀=0.13 nM), can be used for research of BAF complex-related disorders.

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