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Results for "

BET family

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Apoptosis (5) c-Myc (2) Epigenetic Reader Domain (25) HIV (1) HSP (1) Interleukin Related (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) Polo-like Kinase (PLK) (1) PROTACs (8) Reference Standards (1) TNF Receptor (1)
By Research Areas:	Cancer (22) Infection (1) Inflammation/Immunology (4) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112090

ABBV-744 Maximum Cited Publications 9 Publications Verification	Epigenetic Reader Domain HIV	Infection Inflammation/Immunology Cancer
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC₅₀ values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .

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-141438

SIM1 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all *BET* family members, with preference for BRD2 degradation (IC₅₀=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity .

HY-134463

NHWD-870 1 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC₅₀=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .

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-117690

dBRD9	PROTACs Epigenetic Reader Domain	Cancer
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-100352

BI-9564 2 Publications Verification	Epigenetic Reader Domain	Cancer
BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family .

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-114416

GS-626510	Epigenetic Reader Domain	Cancer
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with K_d values of 0.59-3.2 nM for BRD2/3/4, with IC₅₀ values of 83 nM and 78 nM foe BD1 and BD2, respectively .

HY-110374

NVS-CECR2-1 1 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC₅₀=47 nM; K_D=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5) .

HY-138623

GSK789	Epigenetic Reader Domain TNF Receptor Interleukin Related	Inflammation/Immunology Cancer
GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases .

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-138563A

(2R,3R)-GSK973	Epigenetic Reader Domain	Others
(2R,3R)-GSK973 is an isomer of GSK973. GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family .

HY-157491

K2-B4-5e	PROTACs Androgen Receptor Epigenetic Reader Domain	Cancer
K2-B4-5e is a E3 ligase KLHDC2-based BRD4 and androgen receptor (AR) degradation PROTAC. K2-B4-5e is capable of inducing rapid and robust degradation of BET-family and AR proteins in cells .

HY-149948

PROTAC BRD3/BRD4-L degrader-2	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with K_i values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .

HY-172562

BTR2004	PROTACs Epigenetic Reader Domain	Cancer
BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236) .

HY-143471

WNY0824 PLK1/BRD4-IN-1	Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Androgen Receptor c-Myc	Cancer
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and *BET* protein families, with IC₅₀ values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .

HY-163543

Progranulin modulator-2	Epigenetic Reader Domain	Neurological Disease
Progranulin modulator-2 (compound 18A) is a bromodomain and extra-terminal domain (BET) inhibitor. Progranulin modulator-2 enhances PGRN expression by targeting members of the *BET* protein family. Progranulin modulator-2 can be used to study the role of *BET* protein in neurodevelopment, neuroplasticity and neurodegeneration .

HY-181867

PROTAC BET Degrader-16	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BET Degrader-16 (Compound A10) is a *BET* PROTAC degrader with a DC₅₀ of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia .

HY-179588

PROTAC BET Degrader-14	PROTACs Epigenetic Reader Domain c-Myc	Cancer
PROTAC BET Degrader-14 is a highly efficient PROTAC targeting *BET* (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC₅₀ = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC₅₀ = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .

HY-181735

BET-IN-30	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML .

HY-100352R

BI-9564 (Standard)	Epigenetic Reader Domain Reference Standards	Cancer
BI-9564 (Standard) is the analytical standard of BI-9564 (HY-100352). This product is intended for research and analytical applications. BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family .

HY-183077

BRD4 degrader-7	Epigenetic Reader Domain Molecular Glues	Cancer
BRD4 degrader-7 (Compound ZZ1) is a CTLH-dependent BRD4 degrader and c-Glue with a DC₅₀ of 489 nM. BRD4 degrader-7 converts to a sulfinic acid derivative inside cells, interacts with the basic pocket of YPEL5, mediates the bridging of BRD4 BD1 to the YPEL5 subunit of the CTLH E3 ubiquitin ligase, and thereby promotes the formation of a ternary complex. BRD4 degrader-7 can be used in research on Ewing's sarcoma and leukemia .

HY-155891

BET-IN-18	Epigenetic Reader Domain	Cancer
BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with K_i values of 0.69 μM and 0.37 μM, and K_d values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC₅₀ values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC₅₀ = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma .

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BET family

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