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Droxinostat (NS 41080) is a histonedeacetylase(HDAC) inhibitor. Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively. Droxinostat can be used for the research of hepatocellular carcinoma (HCC) .
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histonedeacetylase(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 .
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histonedeacetylase(HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
OKI-006 is a potent and orally active inhibitor of histonedeacetylase(HDAC). OKI-006 is a unique congener of the natural product HDAC inhibitor largazole. Histonedeacetylases (HDACs) play critical roles in epigenomic regulation, and histone acetylation is dysregulated in many human cancers. OKI-006 has the potential for the research of cancer disease .
HDAC6-IN-41 (Compound E24) is a selective inhibitor for histonedeacetylase 6 (HDAC6), with IC50 of 14 and 422 nM, for HDAC6 and HDAC8, respectively. HDAC6-IN-41 upregulates the acetylation of α-tubulin and histone site SMC3 .
BG47 is a prototypical histonedeacetylasesHDAC1 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. BG47 can be used for neurological disease research .
ITSA-1 is an activator of histonedeacetylase(HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
TMP269 is a novel and selective class IIa histonedeacetylase(HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
HDAC6-IN-46 (compound 12) is a selective histonedeacetylase 6 (HDAC6) inhibitor with an IC50 value of 6.2 nM. HDAC6-IN-46 can be used in Alzheimer's disease research .
HDAC-IN-65 ( compound 6) is a selectivehistonedeacetylase(HDAC) inhibitor with IC50 value of 2.5μM. HDAC-IN-65 is a prodrug with very good bioreductive properties .
HDAC-IN-82 (Compound 18b) is a histonedeacetylase(HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin .
HDAC6-IN-38 (Compound Z-7) is an inhibitor for histonedeacetylase 6 (HDAC6), with an IC50 of 3.25 nM. HDAC6-IN-38 inhibits proliferation of cells MGC‑803 .
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histonedeacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase(HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histonedeacetylasesHDAC1 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 .
HDAC8-IN-13 is a novel histonedeacetylase 8 (HDAC8) inhibitor with antiparasitic activity. HDAC8-IN-13 can effectively inhibit the acetyl-L-lysine deacetylase activity of schistosomes, affecting the parasite's infectivity. HDAC8-IN-13 can induce apoptosis and cause the death of schistosome cells. Through a specific structural basis design, HDAC8-IN-13 exhibits reduced affinity for human HDACs, thereby enhancing its selectivity .
SIS17 is a mammalian histonedeacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM. SIS17 inhibits the demyristoylation of serine hydroxymethyltransferase 2, a substrate of HDAC 11, but does not inhibit other HDACs .
HDAC6-IN-15 is a selective histonedeacetylase 6 (HDAC6) inhibitor. HDAC6-IN-15 has potent inhibitory activity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histonedeacetylase (HDAC) activator.
CM-1758 is a histonedeacetylase(HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells .
Pyroxamide is a potent inhibitor of histonedeacetylase 1 (HDAC1) with an ID50 of 100 nM. Pyroxamide can induce apoptosis and cell cycle arrest in leukemia .
(R)-Dihydrolipoic acid is a compound that inhibits histonedeacetylase 6 (HDAC6) activity. The structure of its complex with HDAC6 has been resolved. (R)-Dihydrolipoic acid can inhibit HDAC6 through specific interactions, providing a basis for understanding the relationship between HDAC function and oxidative stress.
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histonedeacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma .
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histonedeacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6).HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
NL-103 is an inhibitor of histonedeacetylases(HDACs) and Hedgehog, with the IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. NL-103 can downregulate the expression of Gli2. NL-103 can be used in anti-cancer research .
Scriptaid is a potent histonedeacetylase(HDAC) inhibitor, used in cancer research. Scriptaid is also a sensitizer to antivirals and has potential for epstein-barr virus (EBV)-associated lymphomas treatment.
Crebinostat is a potent histonedeacetylase(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 .
HDAC6-IN-16 (compound 5c) is a histonedeacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis .
FITC-SAHA is SAHA (HY-10221) conjugated with fluorescein. SAHA is an inhibitor of histonedeacetylase(HDAC). FITC-SAHA can be used in cancer and Alzheimer's disease related research .
HDAC-IN-57 is an orally active inhibitor of histonedeacetylases(HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity .
Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histonedeacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research .
L-Pyrohomoglutamic acid is an amino acid building block. L-Pyrohomoglutamic acid can be used to synthesize ligands for FK506-binding proteins (FKBPs) and histonedeacetylase (HDAC) inhibitors .
SW-100, a selective histonedeacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier .
HDAC-IN-59 (compound 13a) is a potent histonedeacetylase(HDAC) inhibitor. HDAC-IN-59 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
HDAC-IN-60 (compound 21a) is a potent histonedeacetylase(HDAC) inhibitor. HDAC-IN-60 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
HDAC-IN-51 is a potent histonedeacetylase(HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer .
HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor, with IC50 values of 0.27 and 0.32 μM for smHDAC8 (Schistosoma mansonihistonedeacetylase 8) and hHDAC8, respectively. HDAC8-IN-2 shows significant killing of the schistosome larvae. HDAC8-IN-2 markedly impairs egg laying of adult worm pairs .
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase(HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
Butyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histonedeacetylase(HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies .
MC2625 is a potent pyridine-containing histonedeacetylase(HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction .
Romidepsin (FK 228) is a Histonedeacetylase(HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
NKL 22 (compound 4b) is a potent and selective inhibitor of histonedeacetylases(HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC50≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice .
BRD-6929 is a?potent, selective brain-penetrant inhibitor of class I histonedeacetylaseHDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with?Ki?of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research .
BRD4097 is an inhibitor of histonedeacetylase (HDAC). BRD4097 acts by inhibiting the activity of HDACs, especially HDAC 1,2 and 3, through metal chelation and spatial rejection mechanisms, and this inhibition may help regulate gene expression and alter chromatin structure, thereby affecting a variety of biological processes. BRD4097 is used to study the role of HDAC in cholesterol metabolism and NPC1 diseases .
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histonedeacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histonedeacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histonedeacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histonedeacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histonedeacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
HDAC3-IN-T247 is a potent and selective HDAC3 (histonedeacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells .
HDAC-IN-47 is an orally active inhibitor of histonedeacetylase(HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 (HDAC6) with an IC50 of 7.5 nM . ACY775 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
Largazole ((+)-Largazole) is a potent and selective histonedeacetylase (HDAC) inhibitor with antiproliferative activity. Largazole is able to modulate gene expression and affect cell growth and differentiation. Largazole has also shown potential application value in anti-tumor suppression .
PTG-0861 is a selective histonedeacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers .
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histonedeacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases
the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histonedeacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histonedeacetylase (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 .
Pracinostat is a potent histonedeacetylase(HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM .
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histonedeacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease .
Pracinostat dihydrochloride is a potent histonedeacetylase(HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat dihydrochloride also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM .
HDAC-IN-56 ((S)-17b) is an orally active class I histonedeacetylase(HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
TMU 35435 is a histonedeacetylase(HDAC) inhibitor. TMU-35435 inhibits the NHEJ pathway through ubiquitination of DNA-dependent protein kinase catalytic subunit (DNA-PKcs). In addition, TMU 35435 enhances radiosensitivity by inducing misfolded protein aggregation and autophagy in TNBC .
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histonedeacetylase(HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histonedeacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
HNHA is a potent histonedeacetylase(HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer .
ZYJ-25e is a potent histonedeacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
MC2590 is a potent pyridine-containing histonedeacetylase(HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction .
ST7612AA1 is a histonedeacetylase(HDAC) inhibitor that controls chromatin condensation and DNA transcription by removing acetyl groups from histones. ST7612AA1 is also a potent HIV reactivation inducer, and its reactivation activity is exerted without activating or proliferating CD4+T cells, and can be used in the study of HIV reactivation strategies and elimination of viral reservoirs .
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/HistoneDeacetylases(GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
HDAC-IN-76 (compound 6i) is a histonedeacetylase(HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
KBH-A42 is a novel histonedeacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC50 values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells .
HDAC-IN-73 (compound P-503) is a histonedeacetylase(HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
BG14 is a chemical optical modulation of epigenetic regulation of transcription (COMET) probe. BG14 enables high-resolution optical control of epigenetic mechanisms using visible light and can photochromically inhibit human histonedeacetylases(HDACs). BG14 can be used to study the dynamic regulation of the human genome .
Trichostatin C is an inhibitor for histonedeacetylase(HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
AN-7 is an orally active histonedeacetylase(HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
NT376 is a high potency and selectivity inhibitor of class-IIa Histonedeacetylases(HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
H8-A5 is a novel human histonedeacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
HL23 is a histonedeacetylase (HDAC) inhibitor with activity against hepatocellular carcinoma (HCC). HL23 enhances acetylation of the TXNIP promoter and upregulates TXNIP expression, thereby mediating potassium channel activity and triggering TXNIP-dependent potassium deprivation. HL23 inhibits HCC progression and metastasis and has a synergistic effect with Sorafenib (HY-10201) and is more potent than Sorafenib+Vorinostat (HY-10221) .
SelSA is a selective, orally active inhibitor for histonedeacetylase 6(HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
J208 is a dual inhibitor for histonedeacetylase(HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
ZYJ-34c is an orally active and potent histonedeacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells .
4-Iodo-SAHA (1k) is an orally active class I and class II histonedeacetylase(HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline (Compound 11 and 15) is a building block and synthetic intermediate, which can be used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histonedeacetylase (HDAC) inhibitors, and anticancer agents. 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline can also be used to synthesize EGFR inhibitors, including Erlotinib (HY-50896), with antiproliferative activity .
ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histonedeacetylase(HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histonedeacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1 .
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histonedeacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histonedeacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research .
Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Largazole ((+)-Largazole) is a potent and selective histonedeacetylase (HDAC) inhibitor with antiproliferative activity. Largazole is able to modulate gene expression and affect cell growth and differentiation. Largazole has also shown potential application value in anti-tumor suppression .
Trichostatin C is an inhibitor for histonedeacetylase(HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
The HDAC8 protein is a histone deacetylase that has been shown to be critical for lysine deacetylation on core histones (H2A, H2B, H3, H4). This enzymatic activity initiates epigenetic repression that affects transcription, cell cycle, and developmental events. HDAC8 Protein, Human (sf9) is the recombinant human-derived HDAC8 protein, expressed by Sf9 insect cells , with no tag.
The HDAC6 protein coordinates multiple functions, deacetylating histones and proteins such as tubulin and CTTN. Its role in epigenetic repression affects transcription, cell cycle, and development. HDAC6 Protein, Human (His) is the recombinant human-derived HDAC6 protein, expressed by E. coli , with N-6*His labeled tag. The total length of HDAC6 Protein, Human (His) is 352 a.a., with molecular weight of ~42.4 kDa.
Studies have confirmed that the histone deacetylase 1 (HDAC1) protein is a key enzyme that deacetylates lysine residues on core histones (H2A, H2B, H3, H4). This process establishes an epigenetic repressive signature that affects transcription, cell cycle, and developmental events. Histone deacetylase 1/HDAC1 Protein, Human (His-SUMO) is the recombinant human-derived Histone deacetylase 1/HDAC1 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of Histone deacetylase 1/HDAC1 Protein, Human (His-SUMO) is 482 a.a., with molecular weight of ~71-74 kDa.
The HDAC8 protein is a histone deacetylase that removes acetyl groups from core histone lysine residues, contributing to epigenetic repression and affecting transcriptional regulation, cell cycle progression, and developmental events. It forms large multiprotein complexes and deacetylates SMC3, regulating the release of cohesin complexes. HDAC8 Protein, Mouse (sf9, His) is the recombinant mouse-derived HDAC8 protein, expressed by Sf9 insect cells , with C-His labeled tag.
HDAC10 Protein, Human (His) is the recombinant human-derived HDAC10, expressed by E. coli , with N-6*His labeled tag. The total length of HDAC10 Protein, Human (His) is 669 a.a.,
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histonedeacetylase (HDAC) activator.
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histonedeacetylase(HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
HDAC2 Antibody (YA742) is a non-conjugated and Mouse origined monoclonal antibody about 55 kDa, targeting to HDAC2 (2D9). It can be used for WB,ICC/IF assays with tag free, in the background of Human, Mouse, Rat, Monkey.
HDAC11 Antibody (YA2884) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2884), targeting HDAC11, with a predicted molecular weight of 39 kDa (observed band size: 39 kDa). HDAC11 Antibody (YA2884) can be used for WB, IP experiment in human background.
HDAC9 Antibody (YA2967) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2967), targeting HDAC9, with a predicted molecular weight of 111 kDa (observed band size: 150 kDa). HDAC9 Antibody (YA2967) can be used for WB, IHC-P experiment in human background.
HDAC8 Antibody (YA2994) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2994), targeting HDAC8, with a predicted molecular weight of 42 kDa (observed band size: 42 kDa). HDAC8 Antibody (YA2994) can be used for WB, IP experiment in human background.
HDAC4 Antibody (YA741) is a non-conjugated and Mouse origined monoclonal antibody about 119 kDa, targeting to HDAC4 (4A3). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat, Monkey.
HDAC7 Antibody (YA3146) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3146), targeting HDAC7, with a predicted molecular weight of 103 kDa (observed band size: 124 kDa). HDAC7 Antibody (YA3146) can be used for WB, FC experiment in human, mouse, rat background.
HDAC6 Antibody (YA740) is a non-conjugated and Mouse origined monoclonal antibody about 131 kDa, targeting to HDAC6 (3B2). It can be used for WB assays with tag free, in the background of Human, Rat.
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