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Results for "

histone acetylation

" in MedChemExpress (MCE) Product Catalog:

34

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100671
    L002

    		Histone Acetyltransferase STAT Inflammation/Immunology Cancer
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
    L002
  • 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 .
    Triciferol
  • HY-144315
    Snail/HDAC-IN-1

    		HDAC Cancer
    Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 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. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
    Snail/HDAC-IN-1
  • HY-100508
    ITSA-1
    10+ Cited Publications

    		 HDAC Cancer
    ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
    ITSA-1
  • HY-161149
    CM-1758

    		HDAC Cancer
    CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells .
    CM-1758
  • HY-154944
    JG-2016

    		Histone Acetyltransferase Cancer
    JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1), with an IC50 of 14.8 μM in the HAT1 acetylation assays .
    JG-2016
  • HY-144893
    OKI-006

    		HDAC Cancer
    OKI-006 is a potent and orally active inhibitor of histone deacetylase (HDAC). OKI-006 is a unique congener of the natural product HDAC inhibitor largazole. Histone deacetylases (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 .
    OKI-006
  • HY-18935
    CBL0137

    Curaxin 137; CBL-C137
    CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis .
    CBL0137
  • HY-W013274
    CPTH2

    		Histone Acetyltransferase Apoptosis Cancer
    CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .
    CPTH2
  • HY-W013274A
    CPTH2 hydrochloride

    		Histone Acetyltransferase Apoptosis Cancer
    CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .
    CPTH2 hydrochloride
  • HY-109109
    Alteminostat

    CKD-581

    		 HDAC Apoptosis Cancer
    Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research .
    Alteminostat
  • HY-130538
    1-Naphthohydroxamic acid

    		HDAC Cancer
    1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity .1-Naphthohydroxamic acid can induce tubulin acetylation .
    1-Naphthohydroxamic acid
  • HY-163368
    HDAC6-IN-34

    		HDAC Inflammation/Immunology
    HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
    HDAC6-IN-34
  • HY-P5285
    Lunasin

    		Parasite Infection Inflammation/Immunology Cancer
    Lunasin is a bioactive peptide with antioxidant, anti-inflammatory, anticancer and anti-aging properties. Lunasin can be isolated from soybean. Lunasin also has an epigenetic mechanism of action associated with histone acetylation. Lunasin can be internalized into cells and inhibit Oncosphere formation in cancer cells .
    Lunasin
  • 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 .
    cis-BG47
  • 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 .
    Crebinostat
  • HY-N0005
    Curcumin
    Maximum Cited Publications
    62 Publications Verification

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    		 Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin
  • HY-100734
    Histone Acetyltransferase Inhibitor II

    		Histone Acetyltransferase Cancer
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells .
    Histone Acetyltransferase Inhibitor II
  • HY-N2345
    Procyanidin B3

    		Histone Acetyltransferase Cancer
    Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase) .
    Procyanidin B3
  • HY-154993
    Gamma-Glutamyl Transferase-IN-1

    		Others Infection
    Gamma-Glutamyl Transferase-IN-1 (compound 4de) is a β-carboline 1-hydrazide inhibitor with antifungal and antibacterial activities, targeting to glutamyltransferase. Gamma-Glutamyl Transferase-IN-1 acts function by resulting the accumulation of reactive oxygen species, destruction of cell membranes, and dysregulation of histone acetylation .
    Gamma-Glutamyl Transferase-IN-1
  • HY-154996
    Gamma-Glutamyl Transferase-IN-2

    		Others Infection
    Gamma-Glutamyl Transferase-IN-2 (compound 4dq) is a β-carboline 1-hydrazide inhibitor with antifungal and antibacterial activities, targeting to glutamyltransferase. Gamma-Glutamyl Transferase-IN-2 acts function by resulting the accumulation of reactive oxygen species, destruction of cell membranes, and dysregulation of histone acetylation .
    Gamma-Glutamyl Transferase-IN-2
  • HY-162060
    YPX-C-05

    		HDAC Cardiovascular Disease
    YPX-C-05 is a hydroxamic acid-based HDAC inhibitor. YPX-C-05 exerts significant vasodilatory effects. YPX-C-05 exhibits inhibitory effects on HDACs and increases histone H4 acetylation in endothelial cells. YPX-C-05 can be used for hypertension research .
    YPX-C-05
  • HY-10226
    JNJ-16241199

    R306465

    		 Apoptosis HDAC Cancer
    JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (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 .
    JNJ-16241199
  • HY-117617
    CAY10669

    		Histone Acetyltransferase Cancer
    CAY10669 (compound 6d) is an anacardic acid (HY-N2020) derivative that inhibits histone acetyltransferase PCAF with an IC50 of 662 μM . CAY10669 enhances the SAHA-induced acetylation in HEPG2 cells, exhibits cytotoxicity in zebrafish embryo, promotes transgene expression in CHO-K1 cells .
    CAY10669
  • HY-117709
    BRD6688

    		HDAC Neurological Disease
    BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .
    BRD6688
  • HY-155248
    HL23

    		HDAC Cancer
    HL23 is a histone deacetylase (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) .
    HL23
  • HY-100748
    Zabadinostat
    1 Publications Verification

    CXD101

    		 HDAC Cancer
    Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity .
    Zabadinostat
  • HY-146750
    HDAC-IN-37

    		HDAC Apoptosis Cancer
    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 .
    HDAC-IN-37
  • HY-146351
    HDAC-IN-38

    		HDAC Neurological Disease
    HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .
    HDAC-IN-38
  • HY-149306
    MS78

    		Histone Acetyltransferase MDM-2/p53 Cancer
    MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .
    MS78
  • HY-116673
    TTK21

    		Histone Acetyltransferase Neurological Disease
    TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
    TTK21
  • HY-123295
    HDAC3-IN-T247

    		HDAC Infection Cancer
    HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 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 .
    HDAC3-IN-T247
  • HY-151153
    HDAC1-IN-5

    		HDAC Microtubule/Tubulin Caspase Apoptosis Cancer
    HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
    HDAC1-IN-5
  • HY-W015239
    KAT8-IN-1

    		Others Inflammation/Immunology Cancer
    KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases .
    KAT8-IN-1

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