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BRD4 ligand

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E3 Ligase Ligand-Linker Conjugates (7) Target Protein Ligand-Linker Conjugates (2) Apoptosis (3) Autophagy (1) Epigenetic Reader Domain (51) Estrogen Receptor/ERR (1) FKBP (1) Hippo (MST) (1) Ligands for Target Protein for PROTAC (11) Molecular Glues (2) PROTACs (42)
By Research Areas:	Cancer (63) Inflammation/Immunology (1)
Click Chemistry:	Azide (2) Tetrazine (1) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-161651A

BRD4 ligand 6 TFA	Epigenetic Reader Domain	Cancer
BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a *BRD4* ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .

HY-132943A

BRD4 ligand-Linker Conjugate 1 TFA	Target Protein Ligand-Linker Conjugates	Cancer
BRD4 ligand-Linker Conjugate 1 TFA (compound 106-1) is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs .

HY-132942A

*PROTAC BRD4* ligand-2 hydrochloride**	Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-2 hydrochloride is a ligand for target BRD4 protein for PROTAC CFT-2718.

HY-129939

*PROTAC BRD4* ligand-1**	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target *BRD4* protein for PROTACT GNE-987 (HY-129937A) .

HY-161651

BRD4 ligand 6	Epigenetic Reader Domain	Cancer
BRD4 ligand 6 is a *BRD4* ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .

HY-132943

BRD4 ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
BRD4 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs.

HY-132942

*PROTAC BRD4* ligand-2**	Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.

HY-162876

*PROTAC BRD4* ligand-3**	Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC BRD4 ligand-3 can be used for synthesis PROTAC BRD4 Degrader-27 (HY-162875) .

HY-132130

BRD4 Inhibitor-13	Epigenetic Reader Domain	Inflammation/Immunology Cancer
BRD4 Inhibitor-13 (Compound 2) is a *BRD4* ligand, and can be used for research of cancer, inflammation.

HY-132128

BRD4 Inhibitor-12	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-12 (Compound 9) is a *BRD4* ligand, and can be used for research of cancer, infammation .

HY-111433

BRD4 degrader AT1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4* as a highly selective *Brd4* degrader, with a K_d of 44 nM for Brd4 ^BD2 in cells.

HY-107442

PROTAC BRD4-binding moiety 1	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136) . PROTAC BRD4-binding moiety 1 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-133136

PROTAC BRD4 Degrader-2	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 14.2 nM against BRD4 BD1 .

HY-133131

PROTAC BRD4 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and *BRD4* with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression .

HY-133737

PROTAC BRD4 Degrader-5	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. PROTAC BRD4* Degrader-5 can potent degrade *BRD4* in HER2 positive and negative breast cancer cell lines .

HY-161368

BRD-SF2	PROTACs Epigenetic Reader Domain	Cancer
BRD-SF2 is a *BRD4*-targeted PROTAC degrader (DC₅₀: 17.2 μM) (Blue: VHL ligand, black: linker, pink: BRD4 ligand) .

HY-138555

PROTAC BRD4 Degrader-8	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for BRD4* BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .

HY-138637

PROTAC BRD4 Degrader-14	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 1.8 nM and 1.7 nM for BRD4* BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .

HY-139294

PROTAC BRD4 Degrader-15	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4, with IC₅₀s of 7.2 nM and 8.1 nM for BRD4* BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .

HY-135558

PROTAC BRD4 Degrader-3	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and *BRD4* .

HY-169151

PROTAC BRD4-DCAF1 degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4-DCAF1 degrader-1 (I-907) is a *BRD4-DCAF1* PROTAC degrader, DC₅₀ is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)) .

HY-112375

AT6	PROTACs	Cancer
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4* with highly selectivity to bromodomain (Brd4).

HY-161650

PROTAC BRD4 Degrader-26	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% *BRD4* at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))

HY-130612

PROTAC BRD2/BRD4 degrader-1	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein *BRD4* and *BRD2* degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .

HY-107425B

cis-MZ 1 hydrate	Epigenetic Reader Domain	Cancer
cis-MZ 1 hydrate is a negative control for *BRD4*-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The K_d of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively .

HY-138633

PROTAC BRD4 Degrader-10	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. PROTAC BRD4* Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 1.3 nM and 18 nM, respectively .

HY-138632

PROTAC BRD4 Degrader-9	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. PROTAC BRD4* Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.86 nM and 7.6 nM, respectively .

HY-138634

PROTAC BRD4 Degrader-11	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. PROTAC BRD4* Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.23 nM and 0.38 nM, respectively .

HY-138635

PROTAC BRD4 Degrader-12	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. PROTAC BRD4* Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.39 nM and 0.24 nM, respectively .

HY-16954

ARV-825 Maximum Cited Publications 20 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
ARV-825 is a PROTAC connected by ligands for Cereblon and *BRD4. ARV-825 binds to BD1 and BD2 of BRD4* with K_ds of 90 and 28 nM, respectively.

HY-114305

A1874 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
A1874 is a nutlin-based (MDM2 ligand) and *BRD4*-degrading PROTAC with a DC₅₀ of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation .

HY-112718

PROTAC BET Degrader-10	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-10 is a potent BET protein *BRD4* degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and *BRD4, with a DC₅₀* of 49 nM .

HY-130813

BET-IN-6	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
BET-IN-6 is a potent and high affnity *BRD2/BRD4* inhibitor. BET-IN-6 is the *ligand* for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612) .

HY-130814

Thalidomide-NH-C4-NH2 TFA	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .

HY-162875

PROTAC BRD4 Degrader-27	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC *BRD4* Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC *BRD4* ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875) ^{[1] ^.}

HY-112398

GSK1379725A	Epigenetic Reader Domain	Others
GSK1379725A is a selective BPTF ligand with a K_d of 2.8 uM, showing no binding activity for Brd4 .

HY-112609

QCA570	PROTACs Epigenetic Reader Domain	Cancer
QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 10 nM for BRD4 BD1 Protein.

HY-107425

MZ 1 15+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4* over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively .

HY-139620

MS83	PROTACs	Cancer
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

HY-101460

Tz-Thalidomide	PROTACs Molecular Glues Epigenetic Reader Domain	Cancer
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-112376

MZP-54 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD3/4, with a K_d* of 4 nM for Brd4 ^BD2.

HY-112377

MZP-55 1 Publications Verification	Epigenetic Reader Domain PROTACs	Cancer
MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD3/4, with a K_d* of 8 nM for Brd4 ^BD2.

HY-114407

TD-428	PROTACs Epigenetic Reader Domain	Cancer
TD-428 is a PROTAC connected by ligands for Cereblon and *BRD4. TD-428 is a highly specific BRD4* degrader with a DC₅₀?of?0.32?nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .

HY-169152

DCAF1 ligand 1	Ligands for Target Protein for PROTAC	Others
DCAF1 ligand 1 (compound I-653) is the ligand for target protein for PROTAC BRD4-DCAF1 degrader-1 (HY-169151) which has a DC₅₀ of 10~100 nM .

HY-103633

PROTAC BET Degrader-1 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

HY-169358

L134	PROTACs Epigenetic Reader Domain	Cancer
L134 is a potent PROTAC BRD4 degrader with a DC₅₀ value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)) .

HY-129937A

GNE-987 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and *BRD4. GNE-987 exhibits picomolar cell BRD4* degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .

HY-139620A

MS83 epimer 1	PROTACs	Others
MS83 epimer 1 is the epimer of MS83 (HY-139620). MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder .

HY-101838

dBET1 10+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
dBET1 is a PROTAC connected by ligands for Cereblon and *BRD4* with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker .

HY-170383

CCW16-C4-NHBoc	E3 Ligase Ligand-Linker Conjugates	Others
CCW16-C4-NHBoc (RNF4 ligand CCW16 (HY-143346)) is an E3 Ligase Ligand-Linker Conjugate for *BRD4* PROTAC CCW 28-3 (HY-156774) .

Cat. No.	Product Name		Classification

HY-107442

PROTAC BRD4-binding moiety 1		Alkynes
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136) . PROTAC BRD4-binding moiety 1 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-101460

Tz-Thalidomide		Tetrazine
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-133139

Lenalidomide-PEG1-azide		Azide
Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-133138

Pomalidomide-PEG1-azide		Azide
Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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