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Submitted URL: http://www.medchemexpress.com//targets//hdac.html
Effective URL: https://www.medchemexpress.com/search.html?q=/targets//hdac&ft=&fa=&fp=
Submission: On September 17 via api from US — Scanned from DE

Form analysis 3 forms found in the DOM

Name: searchInfo /search.html

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Name: ftr_letterPOST /mce_search.shtml

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Search Result



Results for "


/TARGETS//HDAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:
HDAC (30) Ligands for Target Protein for PROTAC (1) Adenosine Receptor (1) Akt
(1) Apoptosis (9) Caspase (2) DNA Methyltransferase (1) DNA/RNA Synthesis (1)
Estrogen Receptor/ERR (1) G-quadruplex (1) Histone Demethylase (1) Histone
Methyltransferase (2) JAK (2) Microtubule/Tubulin (1) Oxidative Phosphorylation
(1) PARP (2) PROTACs (6) Reactive Oxygen Species (1) Topoisomerase (1) VD/VDR
(1)


By Research Areas: Cancer (27) Cardiovascular Disease (1)
Inflammation/Immunology (1) Neurological Disease (2)

31


INHIBITORS & AGONISTS



2


SCREENING-BIBLIOTHEKEN



1


FLUORESCENT DYE



1


PEPTIDES



Targets Recommended:
 * HDAC
 * Target Protein Ligand-Linker Conjugates
 * Ligands for Target Protein for PROTAC

Art. -Nr. Produktname Target Forschungsgebiete Chemical Structure

 * HY-18712
   BG45
   3 Publications Verification
   
   
   
   HDAC Apoptosis Caspase Cancer BG45 is a potent HDAC3 inhibitor with IC50
   values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6,
   respectively. BG45 selectively targets multiple myeloma (MM) cells and
   induces caspase-dependent apoptosis .

 * HY-163921
   HDAC8-IN-11
   
   
   
   Ligands for Target Protein for PROTAC Cancer HDAC8-IN-11 is a ligand for
   target protein for pROTAC.

 * HY-162349
   PARP7/HDACs-IN-1
   
   
   
   HDAC PARP Cancer PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor
   targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits
   different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM
   (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM
   respectively. (HDAC6) . br/ .

 * HY-163846
   HDAC8-IN-10
   
   
   
   HDAC Cancer HDAC8-IN-10 (compound 15) is a potent inhibitor of HDAC8, with
   the IC50 of 7.6 nM. HDAC8-IN-10 is a HDAC8 target protein ligand that can be
   used to synthesize PROTAC YX862 (HY-163845) .

 * HY-144292
   HDAC-IN-30
   
   
   
   HDAC Cancer HDAC-IN-30 is a novel multi-target HDAC inhibitor, including
   HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6
   (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor
   efficacy .

 * HY-158075
   DNMT/HDAC-IN-1
   
   
   
   HDAC DNA Methyltransferase Cancer DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT
   and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and
   17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in
   tumor research.

 * HY-162319
   Tubulin/HDAC-IN-4
   
   
   
   Apoptosis HDAC Microtubule/Tubulin Reactive Oxygen Species Cancer
   Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with
   IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7,
   respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by
   targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis
   and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant
   elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows
   anti-angiogenesis activity and anticancer activity .

 * HY-149283
   JAK/HDAC-IN-2
   
   
   
   JAK HDAC Apoptosis Cancer JAK/HDAC-IN-2 is a potent
   2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2
   potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has
   proapoptotic activity and inhibits histone deacetylation and STAT3
   phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity
   in both hematological malignancies and solid cancers .

 * HY-146160
   PARP-1/HDAC-IN-1
   
   
   
   PARP HDAC Cancer PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor
   with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays
   remarkable anticancer, anti-migration and anti-angiogenesis activities .

 * HY-151263
   G4/HDAC-IN-1
   
   
   
   HDAC G-quadruplex Cancer G4/HDAC-IN-1 (compound a6) is a G4/HDAC
   dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity
   with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits
   TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can
   be used for the research of cancer .

 * HY-D2280
   Estrogen receptor β/HDAC probe 1
   
   
   
   HDAC Estrogen Receptor/ERR Others Estrogen receptor β/HDAC probe 1 (compound
   P1) is a near-infrared fluorescent probe that dual-targets the estrogen
   receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .

 * HY-124295
   MPT0E028
   
   
   
   HDAC Akt Apoptosis Cancer MPT0E028 is an orally active and selective HDAC
   inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and
   HDAC6, respectively . MPT0E028 reduces the viability of B-cell lymphomas by
   inducing apoptosis and possesses potent direct Akt targeting ability and
   reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer
   activity .

 * HY-145816A
   JPS016 TFA
   
   
   
   HDAC PROTACs Cancer JPS016 is a benzamide-based Von Hippel-Lindau (VHL)
   E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I
   histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with
   greater total differentially expressed genes and enhanced apoptosis in HCT116
   cells .

 * HY-145815
   JPS014
   
   
   
   HDAC PROTACs Cancer JPS014 is a benzamide-based Von Hippel-Lindau (VHL)
   E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I
   histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with
   greater total differentially expressed genes and enhanced apoptosis in HCT116
   cells .

 * HY-145816
   JPS016
   
   
   
   HDAC PROTACs Cancer JPS016 is a benzamide-based Von Hippel-Lindau (VHL)
   E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I
   histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with
   greater total differentially expressed genes and enhanced apoptosis in HCT116
   cells .

 * HY-145818
   JPS035
   
   
   
   HDAC PROTACs Cancer JPS035 is a benzamide-based Von Hippel-Lindau (VHL)
   E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I
   histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with
   greater total differentially expressed genes and enhanced apoptosis in HCT116
   cells .

 * HY-145819
   JPS036
   
   
   
   HDAC PROTACs Cancer JPS036 is a benzamide-based Von Hippel-Lindau (VHL)
   E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I
   histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with
   greater total differentially expressed genes and enhanced apoptosis in HCT116
   cells .

 * HY-116818
   Crebinostat
   
   
   
   HDAC Neurological Disease Crebinostat is a potent histone deacetylase (HDAC)
   inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1,
   HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces
   acetylation of both histone H3 and histone H4 as well as enhances the
   expression of the cAMP response element-binding protein (CREB) target gene
   Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites
   in cultured neurons. Crebinostat can modulate chromatin-mediated
   neuroplasticity and exhibits enhanced memory in mice .

 * HY-10990
   Abexinostat
   Maximum Cited Publications
   6 Publications Verification
   
   CRA 024781; PCI-24781
   
   HDAC Cancer Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly
   targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits
   metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity
   with an EC50 below 10 nM .

 * HY-156096
   HDAC3-IN-2
   
   
   
   HDAC Histone Methyltransferase Caspase Apoptosis DNA/RNA Synthesis Cancer
   HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor
   (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells.
   HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of
   0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in
   tumor-bearing mouse models, selectively increasing the acetylation levels of
   H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related
   caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related
   Bcl-2, CD44, EGFR, and Ki-67 levels .

 * HY-145815A
   JPS014 TFA
   
   
   
   PROTACs HDAC Apoptosis Cancer JPS014 TFA is a benzamide-based Von
   Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014
   TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2
   degrader correlated with greater total differentially expressed genes and
   enhanced apoptosis in HCT116 cells .

 * HY-117688
   WJ35435
   
   
   
   HDAC Topoisomerase Apoptosis Cancer WJ35435 is a dual-targeted anticancer
   hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and
   anti-topoisomerase I activities that cause DNA damage associated with a low
   DNA repair capability, and induce cell cycle arrest at G1- and G2-phase to
   apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation,
   α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect.
   WJ35435 is promising for research of cancer .

 * HY-117583
   cis-BG47
   
   
   
   HDAC Histone Methyltransferase Neurological Disease cis-BG47 is an cis-isomer
   of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2
   selective, optoepigenetic probe. BG47 can bind to and competitively inhibits
   the deacetylase activity of HDAC targets upon a light-induced trans-to-cis
   isomerization, and increases Histone Methyltransferase H3K9 acetylation.
   cis-BG47 can be used for neurological disease research .

 * HY-156094
   JMJD3/HDAC-IN-1
   
   
   
   HDAC Histone Demethylase Apoptosis Cancer JMJD3/HDAC-IN-1 (compound A5b) is a
   dual inhibitor targeting Jumonji domain-containing protein demethylase 3
   (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes
   hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also
   cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively
   inhibits cancer cell cloning, migration, and invasion .

 * HY-126147
   J22352
   
   
   
   HDAC Cancer J22352 is a PROTAC (proteolysis-targeting chimeras)-like and
   highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352
   promotes HDAC6 degradation and induces anticancer effects by inhibiting
   autophagy and eliciting the antitumor immune response in glioblastoma
   cancers, and leading to the restoration of host antitumor activity by
   reducing the immunosuppressive activity of PD-L1 .

 * HY-144315
   CYD19
   
   Snail/hdac-IN-1
   
   HDAC Cancer CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19
   displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM
   and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases
   histone H4 acetylation in HCT-116 cells and decreases the expression of Snail
   protein to induce cell apoptosis .

 * HY-149718
   Antitumor agent-123
   
   
   
   JAK HDAC Cancer Antitumor agent-123 (Copmound 4d) effectively inhibits
   multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1
   and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3,
   respectively. Antitumor agent-123 exhibits moderate activity in solid tumor
   models .

 * HY-145406
   IHCH-3064
   
   
   
   Adenosine Receptor HDAC Inflammation/Immunology Cancer IHCH-3064 is a
   dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064
   exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1
   (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines
   in vitro. IHCH-3064 is a tumor immunotherapeutic agent.

 * HY-106409
   Tefinostat
   1 Publications Verification
   
   CHR-2845
   
   HDAC Apoptosis Cancer Tefinostat (CHR-2845) is a monocyte/macrophage targeted
   histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active
   acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1).
   Tefinostat can be used for the research of leukaemias .

 * HY-153392
   TYA-018
   
   
   
   Oxidative Phosphorylation HDAC Cardiovascular Disease TYA-018 is an orally
   active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect
   heart function in mice. TYA-018 also enhances energetics in mice by
   increasing expression of targets associated with fatty acid metabolism,
   protein metabolism, and oxidative phosphorylation .

 * HY-131961
   Triciferol
   
   
   
   VD/VDR HDAC Cancer Triciferol functions as a multiple ligand with combined
   VDR agonist and HDAC antagonist activities. Triciferol binds directly to the
   VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on
   several 1,25D target genes. Triciferol induces marked tubulin
   hyperacetylation, and augments histone acetylation. Antiproliferative and
   cytotoxic activities .

Art. -Nr. Produktname

 * HY-L024
   Histone Modification Research Compound Library
   669 compounds
   
   A histone modification, a covalent post-translational modification (PTM) to
   histone proteins, includes methylation, phosphorylation, acetylation,
   ubiquitylation, and sumoylation, etc. In general, histone modifications are
   catalyzed by specific enzymes that act predominantly at the histone
   N-terminal tails involving amino acids such as lysine or arginine, as well as
   serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene
   expression by altering chromatin structure or recruiting histone modifiers.
   Histone modifications act in diverse biological processes such as
   transcriptional activation/inactivation, chromosome packaging, and DNA
   damage/repair. Deregulation of histone modification contributes to many
   diseases, including cancer and autoimmune diseases.
   
   MCE owns a unique collection of 669 bioactive compounds targeting Epigenetic
   Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone
   Methyltransferase, Sirtuin, etc. Histone Modification Research Compound
   Library is a useful tool for histone modification research and drug
   screening.

 * HY-L005
   Epigenetics Compound Library
   1,325 compounds
   
   Epigenetics refers to changes in phenotype that are not rooted in DNA
   sequence. Many types of epigenetic processes have been identified, including
   DNA methylation, alteration in the structure of histone proteins and gene
   regulation by small noncoding microRNAs. Modification of DNA, protein, or
   RNA, resulting in changes to the function and/or regulation of these
   molecules, without altering their primary sequences, reveals the complexities
   of cellular differentiation, embryology, the regulation of gene expression,
   aging, cancer, and other diseases.
   
   MCE provide a unique collection of 1,325 epigenetics-related compounds that
   can be used in the research of the related diseases.

Art. -Nr. Produktname Type

 * HY-D2280
   Estrogen receptor β/HDAC probe 1
   
   
   
   Fluorescent Dyes/Probes Estrogen receptor β/HDAC probe 1 (compound P1) is a
   near-infrared fluorescent probe that dual-targets the estrogen receptor
   (Estrogen Receptor/ERR) β/histone deacetylase HDAC .

Art. -Nr. Produktname Target Research Area

 * HY-144292
   HDAC-IN-30
   
   
   
   HDAC Cancer HDAC-IN-30 is a novel multi-target HDAC inhibitor, including
   HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6
   (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor
   efficacy .





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