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Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
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 .
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 .
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 .
APHA Compound 8 (Compound 4) is a histonedeacetylase (HDAC) inhibitor. APHA Compound 8 has antimouse HDAC1 activity with an IC50 value of 0.78 μM. APHA Compound 8, as antiproliferative and cytodifferentiating agent on MEL cells, shows dose-dependent growth inhibition and hemoglobin accumulation effects .
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 .
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) .
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 .
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) .
YF479 is a potent inhibitor of histonedeacetylase. YF479 abates cell viability, suppresses colony formation and tumor cell motility. YF479 significantly inhibits breast tumor growth and metastasis. YF479 has the potential for the research of clinical trials for breast 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 .
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 .
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 .
ITSA-1 is an activator of histonedeacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
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 .
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.
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histonedeacetylase (HDAC) activator.
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 .
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 .
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 .
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.
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.
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
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 .
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 .
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.
SIS17 is a mammalian histonedeacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs .
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) .
RSC133 exhibits dual activity by inhibiting histonedeacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells .
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 .
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 .
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 .
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 .
Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity . Quisinostat can induce autophagy in neuroblastoma cells .
Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity .
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 .
JNJ-16241199 is an orally active, selective hydroxamate-based histonedeacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
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 .
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 .
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 .
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 .
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 .
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 .
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 (HADC1, 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 .
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 .
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) .
HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions .
HDAC6-IN-17 (compound 5b) is a potent HDAC6 inhibitor with IC50 values of 150 nM, 1400 nM, and 2300 nM for HDAC6, HDAC8, and HDAC4, respectively. HDAC6-IN-17 has cytotoxic activity on human cancer cell lines. HDAC6-IN-17 can be used in research of cancer .
HDAC6-IN-31 (compound 8m) is a selective HDAC6 inhibitor, with the IC50 value of 0.026 μM, that significantly inhibits the production and release of pro-inflammatory cytokines. While HDAC6 is critically involved in the activation of inflammasomes, HDAC6-IN-31 has the potential to inhibit NLRP3 inflammasome-driven inflammatory diseases. HDAC6-IN-31 also inhibits glioblastoma cell migration .
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
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 .
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 .
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 .
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 .
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity .
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity .
Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
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 .
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis .
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
HDAC-IN-67 (compound 27f) is an HDAC inhibitor against HDAC1 and HDAC6, with IC50 values of 22 nM and 8 nM, respectively. HDAC-IN-67 inhibits cell proliferation and induces cell apoptosis. HDAC-IN-67 exhibits antitumor activity .
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 .
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 .
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 Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
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 .
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 .
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC50s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe2+ and Cu2+). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.
HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion .
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
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 .
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 .
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 (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 .
The HDAC4 protein deacetylates core histones, thereby affecting transcription, cell cycle, and development. During muscle maturation, HDAC4 interacts with myocyte enhancer factors (MEF2A, MEF2C, and MEF2D). HDAC4 Protein, Human (sf9) is the recombinant human-derived HDAC4 protein, expressed by Sf9 insect cells , with tag free. The total length of HDAC4 Protein, Human (sf9) is 473 a.a., with molecular weight of ~51 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. The total length of HDAC8 Protein, Mouse (sf9, His) is 377 a.a., with molecular weight of ~46 kDa.
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, GST) is the recombinant human-derived HDAC8 protein, expressed by Sf9 insect cells , with C-GST labeled tag. The total length of HDAC8 Protein, Human (sf9, GST) is 377 a.a., with molecular weight of ~68 kDa.
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-SUMO) is the recombinant human-derived HDAC6 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of HDAC6 Protein, Human (His-SUMO) is 488 a.a., with molecular weight of ~70.1 kDa.
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.
Sap130 Protein, a transcriptional repressor, participates in mSin3A corepressor complex assembly or enzymatic activity. It's a component of the complex, including SIN3A, SAP130, SUDS3/SAP45, ARID4B/SAP180, HDAC1, and HDAC2. Sap130 also interacts with CLEC4E, especially when released by dead or dying cells. Sap130 Protein, Mouse (His) is the recombinant mouse-derived Sap130 protein, expressed by E. coli, with N-6*His labeled tag. The total length of Sap130 Protein, Mouse (His) is 213 a.a., with molecular weight of ~34 kDa.
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histonedeacetylase (HDAC) activator.
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.
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.
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.
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
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