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BRD4-PROTAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (1) PROTAC Linkers (1) Apoptosis (2) c-Myc (1) Caspase (1) Drug-Linker Conjugates for ADC (1) E3 Ligase Ligand-Linker Conjugates (3) Epigenetic Reader Domain (26) Ligands for E3 Ligase (2) PD-1/PD-L1 (1) PROTACs (21)
By Research Areas:	Cancer (29) Inflammation/Immunology (1)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: PROTAC Linkers PROTAC-Linker Conjugates for PAC Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114406

TD-106	Ligands for E3 Ligase	Cancer
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 *PROTACs with TD-106 induce BRD4* degradation .

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-131203

PROTAC BRD4 Degrader-6	PROTACs Epigenetic Reader Domain Apoptosis c-Myc Caspase	Cancer
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule *BRD4*PROTAC 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 (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) .

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-168692

3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol	PROTAC Linkers	Others
3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol is a linker for BRD4 PROTAC BD-9136 (HY-149878) .

HY-173435

E3 ligase Ligand 60	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 60 is a ligand for E3 ligase, used for the synthesis of JV8 (HY-173433) .

HY-156566

PROTAC BRD4 Degrader-21	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of *BRD4*. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .

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) .

HY-157561

K2-B4-3e	PROTACs Epigenetic Reader Domain	Cancer
K2-B4-3e is a potent *BRD4* PROTAC. K2-B4-3e induces BRD4 degradation with a DC₅₀ value of 66 nM .

HY-177041

PROTAC BRD4 Degrader-35	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of *BRD4*. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase) .

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-169401

L321-NH-C3-PEG3-C1-NH2	E3 Ligase Ligand-Linker Conjugates	Others
L321-NH-C3-PEG3-C1-NH2 (CRBN ligand L321 (HY-169359)) is an E3 Ligase Ligand-Linker Conjugate for *BRD4* PROTAC L134 (HY-169358) .

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-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-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-174975

JY-21	PROTACs Epigenetic Reader Domain	Cancer
JY-21 is a *BRD4* PROTAC degrader with a DC₅₀ of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells . Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)

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-174210

PROTAC BRD4 Degrader-31	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-31 is a *BRD4* PROTAC degrader with DC₅₀ s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics . Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)

HY-174997

PFI-7-O-C4-piperazin	E3 Ligase Ligand-Linker Conjugates	Cancer
PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162 (HY-174996). The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (KD = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity ^{[1] ^.}

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-170808

PROTAC BRD4 Degrader-28	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting *BRD4*. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)) .

HY-173433

JV8	Epigenetic Reader Domain	Cancer
JV8 is a *BRD4* PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .

HY-175240

PROTAC BRD4 Degrader-38	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-38 is a *BRD4* PROTAC degrader with DC₅₀s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28 .Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)

HY-164995

L1BC8	PROTACs Epigenetic Reader Domain Drug-Linker Conjugates for ADC	Cancer
L1BC8 (compound 13a) is a **BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC** that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)) .

HY-174920

PROTAC BRD4 Degrader-34	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective **BRD4 PROTAC degrader (pDC₅₀** = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)) .

HY-175224

PROTAC BRD4 Degrader-36	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-36 is a **BRD4 PROTAC** degrader. PROTAC BRD4 Degrader-36 has a DC₅₀ of 0.649 nM and a D_max of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI₅₀: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)) .

HY-174811

PROTAC BRD4 Degrader-33	PROTACs Epigenetic Reader Domain PD-1/PD-L1	Inflammation/Immunology Cancer
PROTAC BRD4 Degrader-33 is an enzyme activated clickable *BRD4* PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker

HY-174996

NEP162	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
NEP162 is a BRD4 PROTAC degrader with DC₅₀s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc.(Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)) .

HY-149878

BD-9136	PROTACs Epigenetic Reader Domain	Cancer
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-153519

WWL0245	Epigenetic Reader Domain	Cancer
WWL0245 is a potent and seletive *BRD4* PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC₅₀ (<1 nM) than BRD2/3 and PLK1 ( DC₅₀>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .

HY-176449

PROTAC BRD4 Degrader-32	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-32 (Compound 22) is a *BRD4* PROTAC degrader (DC₅₀: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)) .

HY-176035

MS479	PROTACs Epigenetic Reader Domain	Cancer
MS479 is a **BRD4 PROTAC** degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: K_d = 200 nM; GLP: K_d = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .

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.

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