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Results for "

bromodomain proteins

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HSP (2) Akt (1) Androgen Receptor (1) Antibiotic (1) Apoptosis (7) ATP-binding cassette (ABC) transporters (1) Autophagy (3) Bacterial (1) c-Myc (3) Casein Kinase (1) Deubiquitinase (1) Drug Intermediate (1) Drug Isomer (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (58) FLT3 (1) Fungal (1) HDAC (1) Histone Acetyltransferase (4) Histone Methyltransferase (1) HIV (1) JAK (1) Ligands for Target Protein for PROTAC (5) Molecular Glues (4) PARP (1) Polo-like Kinase (PLK) (1) PROTACs (12) SWI/SNF Complex (1)
By Research Areas:	Cancer (53) Infection (2) Inflammation/Immunology (13) Metabolic Disease (1) Neurological Disease (3)

By Targets:

HSP (2)

Akt (1)

Androgen Receptor (1)

Antibiotic (1)

Apoptosis (7)

ATP-binding cassette (ABC) transporters (1)

Autophagy (3)

Bacterial (1)

c-Myc (3)

Casein Kinase (1)

Deubiquitinase (1)

Drug Intermediate (1)

Drug Isomer (1)

E3 Ligase Ligand-Linker Conjugates (1)

Epigenetic Reader Domain (58)

FLT3 (1)

Fungal (1)

HDAC (1)

Histone Acetyltransferase (4)

Histone Methyltransferase (1)

HIV (1)

JAK (1)

Ligands for Target Protein for PROTAC (5)

Molecular Glues (4)

PARP (1)

Polo-like Kinase (PLK) (1)

PROTACs (12)

SWI/SNF Complex (1)

By Research Areas:

Cancer (53)

Infection (2)

Inflammation/Immunology (13)

Metabolic Disease (1)

Neurological Disease (3)

Targets Recommended: Slit Proteins Synaptic Vesicle Proteins HSP YTHDF

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18975

I-BRD9 Maximum Cited Publications 9 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC₅₀ value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways .

HY-136570

GSK778 1 Publications Verification iBET-BD1	Epigenetic Reader Domain Apoptosis	Inflammation/Immunology Cancer
GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models .

HY-153367

FHD-609 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
FHD-609 is a PROTAC degrader and inhibitor of BRD9 (Bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) ) .

HY-19541

I-CBP112 5 Publications Verification	Histone Acetyltransferase Epigenetic Reader Domain	Cancer
I-CBP112, a chemical probe, is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.

HY-16586

PFI-1 3 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1, a chemical probe, is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-19537

NI-57 1 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology Cancer
NI-57, a chemical probe, is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC₅₀s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.

HY-136571

GSK046 3 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC₅₀s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity .

HY-141539

SETDB1-TTD-IN-1 5 Publications Verification	Histone Methyltransferase Akt	Cancer
SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (K_d of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .

HY-117286

(S)-JQ-35 TEN-010	Epigenetic Reader Domain Apoptosis	Neurological Disease Cancer
(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma .

HY-156214

NICE-01 AP1867-PEG2-JQ1; AP-PEG2-JQ1	Epigenetic Reader Domain	Others
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins .

HY-137892

GSK620	Epigenetic Reader Domain	Inflammation/Immunology
GSK620, a chemical probe, is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .

HY-147868

DC-CPin711	Epigenetic Reader Domain Apoptosis	Cancer
DC-CPin711 is a potent and selective inhibitor of *CREB-binding protein* (CBP)** bromodomain with an IC₅₀ of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis .

HY-19760

I-BET282	Epigenetic Reader Domain	Inflammation/Immunology
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .

HY-112610

CF53	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d of 2.2 nM and an IC₅₀ of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .

HY-W010649

Isoxazole	HSP Epigenetic Reader Domain ATP-binding cassette (ABC) transporters Bacterial Fungal Antibiotic	Infection Metabolic Disease Inflammation/Immunology Cancer
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective *multidrug resistance protein* (MRP1)** inhibitor .

HY-146208

BRD4 Inhibitor-20 1 Publications Verification	Epigenetic Reader Domain	Cancer
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .

HY-145125

SJ995973	PROTACs	Others
SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.

HY-W017851

4-Phenyl-2-pyrrolidinone	Drug Intermediate	Neurological Disease
4-Phenyl-2-pyrrolidinone is a precursor and synthetic intermediate. 4-Phenyl-2-pyrrolidinone can be used as a precursor in the synthesis of compounds with anticonvulsant and nootropic activities and is an intermediate in the synthesis of bromodomain-containing protein 4 (BRD4) bromodomain 1 inhibitors .

HY-112150

ZL0454 2 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC₅₀ of 49 and 32 nM for BD1 and BD2.

HY-130256

β-NF-JQ1	PROTACs Epigenetic Reader Domain	Cancer
β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity .

HY-141890

BAZ1A-IN-1 1 Publications Verification	Epigenetic Reader Domain	Cancer
BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a K_D value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A .

HY-158764

PROTAC BET Degrader-12	PROTACs Epigenetic Reader Domain	Cancer
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-111916

ODM-207 BET-IN-4	Epigenetic Reader Domain	Cancer
ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC₅₀ of ≤ 1 μM .

HY-112149

ZL0420	Epigenetic Reader Domain	Inflammation/Immunology
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

HY-170817

SMI-1074	Ligands for Target Protein for PROTAC SWI/SNF Complex	Cancer
SMI-1074, a SMARCA bromodomain inhibitor, is a PROTAC target protein ligand (*Ligand for Target Protein* for PROTAC*). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828). SMI-1074 can be used for the research of smarca4*-deficient cancers .

HY-123911

dBET23	PROTACs Epigenetic Reader Domain	Cancer
dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC_50/5h of ~ 50 nM for BRD4_BD1 protein .

HY-149420

BRD7-IN-2	Epigenetic Reader Domain	Others
BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 is selective for BRD7 rather than BRD9, with IC50s of 5.4 μM, and >300 μM, respectively.

HY-143332

TRIM24/BRPF1-IN-2	Epigenetic Reader Domain	Cancer
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC₅₀ values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research .

HY-145260

BRD4/CK2-IN-1	Epigenetic Reader Domain Casein Kinase Apoptosis Autophagy	Cancer
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC₅₀s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)

HY-151364

HDAC6/8/BRPF1-IN-1	HDAC	Cancer
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both *HDAC6/8 and the bromodomain* and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC₅₀ values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an K_d** value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .

HY-112149A

(E/Z)-ZL0420	Epigenetic Reader Domain	Inflammation/Immunology Cancer
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC₅₀ values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .

HY-156566

PROTAC BRD4 Degrader-21	PROTACs Epigenetic Reader Domain HSP	Cancer
PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC₅₀ value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC₅₀ of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .

HY-123626

BiBET	Epigenetic Reader Domain	Cancer
BiBET is a chemical probe of BET/BRD4 and is able to bind to two bromodomains simultaneously in a bivalent and cis-binding mode .

HY-12863B

CPI-0610 carboxylic acid	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
CPI-0610 carboxylic acid is a ligand for target protein for PROTACT. CPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma .

HY-157592

MMH2-NR	Molecular Glues Epigenetic Reader Domain	Cancer
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .

HY-19549

RX-37	Epigenetic Reader Domain	Cancer
RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with K_i values of 3.2-24.7 nM. RX-37 can be used for research of cancers .

HY-125051

SG3-179	JAK FLT3	Cancer
SG3-179 is a potent inhibitor against the BET bromodomain proteins. SG3-179 is also a JAK2 and FLT3 inhibitor. SG3-179 causes a rapid reduction in HOXB13 protein expression. SG3-179 is promising for research of multiple myeloma (MM1.S) .

HY-136570A

GSK778 hydrochloride iBET-BD1 hydrochloride	Apoptosis Epigenetic Reader Domain	Inflammation/Immunology Cancer
GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively .

HY-178043

BTR2038	Epigenetic Reader Domain	Others
BTR2038 is a BRD9 degrader. BTR2038 consistis of a BRD9 bromodomain ligand (Bl-7273 analoag), a linker and BTR2000 (HY-172563). BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function .

HY-130853

Thalidomide-NH-PEG2-C2-NH-Boc	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the?Thalidomide?based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology .

HY-177730

PROTAC BRD4 Degrader-40	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))

HY-171774

PBRM1/SMARCA2,4-ligand-1	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a *Ligand for Target Protein* for PROTAC that binds to PBRM1, SMARCA2, and SMARCA4*. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain* inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410) .

HY-161958

dCE-2	PROTACs Histone Acetyltransferase	Cancer
dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) ^{[1] ^.}

HY-175767

PROTAC BRD4 Degrader-39	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC₅₀ value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))

HY-117598

OXFBD03	Epigenetic Reader Domain	Others
OXFBD03 serves as an inhibitor of the BRD4(1) protein, which belongs to the bromodomain and extra terminal domain bromodomain family.

HY-164005

CBP/EP300 bromodomain receptor-IN-1	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CBP/EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor for CBP/EP300 bromodomain receptor, which binds to proteins having a bromodomain in nanomolar level .

HY-122573

Bromodomain inhibitor-13	Epigenetic Reader Domain	Cancer
Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with K_D values of 37, 53, 30, and 190 nM, respectively .

HY-160262

AR/BET protein degrader-1	Androgen Receptor PROTACs Epigenetic Reader Domain	Cancer
AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research .

HY-147869

DC-CPin7	Epigenetic Reader Domain	Cancer
DC-CPin7 is a potent inhibitor of *CREB-binding protein* (CBP)** bromodomain with an IC₅₀ of 2.5 μM .

HY-132232

GSK097	Epigenetic Reader Domain	Cancer
GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media .

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bromodomain proteins

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