Search Result
Results for "
deacetylase activity
" in MedChemExpress (MCE) Product Catalog:
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- HY-15149
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Romidepsin
Maximum Cited Publications
70 Publications Verification
FK 228; FR 901228; NSC 630176
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HDAC
Apoptosis
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Cancer
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Romidepsin (FK 228) is a Histone deacetylase (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 .
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- HY-B0809
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- HY-109521A
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Manganese(Ⅱ) chloride tetrahydrate, molecular biology grade,≥99.0% (KT)
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Biochemical Assay Reagents
Histone Acetyltransferase
HDAC
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Neurological Disease
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Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
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- HY-N6735
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OSI 2040
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HDAC
Parasite
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Infection
Cancer
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Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histone deacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research .
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- HY-13322
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SB939
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Beta-lactamase
HDAC
Apoptosis
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Cancer
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Pracinostat is a potent histone deacetylase (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 .
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- HY-135899
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Sirtuin
Apoptosis
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Cancer
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SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. .
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- HY-15510
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MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
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Cancer
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Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH) .
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- HY-N7036
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- HY-107582
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Ser/Thr Protease
Calcium Channel
PKC
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Cancer
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JW480 is a selective KIAA1363/AADACL1 inhibitor with oral activity, featuring IC50 values of 12 nM against human KIAA1363, 20 nM against mouse KIAA1363. JW480 blocks lipid deacetylase activity to restrain HAG metabolism and lowers retinyl ester hydrolase function in hepatic stellate cells. JW480 reduces MAGE lipid levels and inhibits migration, invasion, survival and tumor growth of prostate cancer cells. JW480 lowers PKCδ phosphorylation, facilitates HAGP accumulation, diminishes platelet aggregation, dense granule secretion and Ca 2+ flux, delays arterial thrombosis and prolongs tail bleeding time in rats. JW480 can be used for the study of prostate cancer and thrombosis .
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- HY-15510B
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MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
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Cancer
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Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH) .
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- HY-107549
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HDAC
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Cancer
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KD 5170 is a pan inhibitor of histone deacetylases (HDACs) and exhibits broad spectrum antitumor activity in vitro and in vivo .
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- HY-B0809A
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1,3-Dimethylxanthine monohydrate; Theo-24 monohydrate
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Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
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Cancer
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Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
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- HY-123295
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HDAC
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Infection
Cancer
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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 .
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- HY-Y1058
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BHA
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Fungal
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Infection
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Benzohydroxamic acid (BHA) is a chitin deacetylase (CDA) inhibitor with significant antifungal activity. The Ki values of BHA against the CDAs of Verticillium dahliae and Puccinia striiformis f. sp. tritici are 8.31 μM and 9.83 μM, respectively. Benzohydroxamic acid can restore the defense responses of infected host plants, upregulate the expression of defense-related genes, and reduce the growth and reproduction of fungi in plants. Benzohydroxamic acid can be used in the research of the field of controlling agricultural fungal diseases, such as various plant fungal diseases caused by Verticillium dahliae, Puccinia striiformis and other fungi, like cotton wilt and wheat stripe rust .
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- HY-155248
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HDAC
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Cancer
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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) .
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- HY-B0809R
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1,3-Dimethylxanthine(Standard); Theo-24 (Standard)
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Reference Standards
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
Endogenous Metabolite
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Cancer
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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 histone deacetylase (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 .
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- HY-156023
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- HY-176545
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HDAC
Sirtuin
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Others
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Z-MAL is a highly efficient and broad-spectrum HDAC substrate. Z-MAL exhibits high conversion activity for class I, II histone deacetylases, and class III SIRT1. Z-MAL can be used in studies on the structure-activity relationship, subtype selectivity, and inhibitor screening of HDAC .
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- HY-162616
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HDAC
Apoptosis
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Cancer
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SelSA is a selective, orally active inhibitor for histone deacetylase 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 .
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- HY-107909
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1,3-Dimethylxanthine sodium glycinate; Theo-24 sodium glycinate
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Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
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Cancer
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Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
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- HY-15149S2
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FK 228-d7; FR 901228-d7; NSC 630176-d7
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Isotope-Labeled Compounds
HDAC
Apoptosis
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Cancer
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Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (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 .
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- HY-15149G
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FK 228; FR 901228; NSC 630176
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HDAC
Apoptosis
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Cancer
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Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (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 .
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- HY-119505
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HDAC
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Others
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Curcuphenol is a compound with histone deacetylase enhancing activity and has the activity of reversing immune escape. Curcuphenol can reverse the immune escape of tumors by restoring the expression of antigen presentation machinery. Its two synthetic analogs have histone deacetylase enhancing activity and play an important role in the immune recognition of metastatic tumors.
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- HY-178350
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CDK
HDAC
Apoptosis
Histamine Receptor
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Cancer
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MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer .
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- HY-126566
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Fungal
HDAC
Apoptosis
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Infection
Cancer
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Trichostatin C is an inhibitor for histone deacetylase (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 .
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- HY-W021291
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Biochemical Assay Reagents
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Cancer
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Butyl isothiocyanate inhibits the proliferation of breast cancer cells. Butyl isothiocyanate can inhibit carcinogen activating phase I enzymes and inhibits cancer cell proliferation through altering the telomerase activity, dynamics of microtubules as well as expression of histone deacetylases. Butyl isothiocyanate can be studied in anti-cancer research .
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- HY-146684
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HDAC
Autophagy
Apoptosis
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Cancer
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HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) 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 .
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- HY-177878
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Sirtuin
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Inflammation/Immunology
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IMU-856 is an orally active and systemic action SIRT6 small molecule regulator. IMU-856 effectively and selectively inhibits the deacetylase activity of SIRT6, while increasing the protein level of SIRT6. IMU-856 can restore intestinal barrier function and can be used for research on celiac disease .
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- HY-W016689
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Drug Intermediate
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Cancer
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2-Amino-4-phenylthiazole is a synthetic intermediate useful for pharmaceutical synthesis. 2-Amino-4-phenylthiazole can be used to synthesize suberoylanilide hydroxamic acid (SAHA) analogs with cancer cell growth inhibitory activities. 2-Amino-4-phenylthiazole also can be used to synthesize ketone histone deacetylase inhibitors with antitumor activity in vivo .
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- HY-179238
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Estrogen Receptor/ERR
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Cancer
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CS-1-103 is a potent estrogen receptor (ER) inhibitor. CS-1-103 inhibits ER transcriptional activity with an EC50 of 0.36 μM by recruiting methyl-CpG binding domain protein 2 (MBD2), HDACs and the nucleosome remodeling and deacetylase (NuRD) complex. CS-1-103 can be used for breast and prostate cancer research .
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- HY-169846
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Sirtuin
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Metabolic Disease
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CL5D is an activator of protein deacetylase SIRT6. CL5D can significantly enhance the deacetylation activity of SIRT6 and improve its catalytic efficiency. CL5D regulates SIRT6 activity by promoting conformational changes, especially dependent on the role of Arg-65 residue. CL5D can be used to study the activation mechanism of SIRT6 and its function in metabolism, DNA repair and aging .
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- HY-131907
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Bacterial
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Infection
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LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively .
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- HY-12926
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HIV
HDAC
DNA/RNA Synthesis
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Infection
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ST7612AA1 is a histone deacetylase (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 .
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- HY-W007977
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Drug Intermediate
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Cancer
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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 histone deacetylase (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 .
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- HY-179272
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Wee1
HDAC
Apoptosis
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Cancer
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Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .
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- HY-161688
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Apoptosis
HDAC
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Cancer
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HDAC-IN-73 (compound P-503) is a histone deacetylase (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 .
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- HY-176866
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HDAC
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Neurological Disease
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Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
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- HY-179227
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HDAC
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Neurological Disease
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HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
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- HY-114737
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Bacterial
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Infection
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L-573655 is a reversible inhibitor of UDP-3-O-[R-3-hydroxymyristoyl]-GlcNAc deacetylase with an IC50 value of 8.5 μM. L-573655 possesses antibacterial activity against a wild-type strain of E. coli. with MIC values of 200-400 μg/mL .
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- HY-126182
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Endogenous Metabolite
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Cardiovascular Disease
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Deacetyldiltiazem is a metabolite with coronary vasodilator activity. Deacetyldiltiazem is present in the plasma of individuals taking Diltiazem. The deacetylase activity of deacetyldiltiazem is mainly catalyzed by the rat Ces2a enzyme. In vitro experiments of deacetyldiltiazem showed that its Km value was similar to that of rat liver microsomes, showing efficient deacetylase activity. The study of deacetyldiltiazem helps to understand the differences in the metabolic kinetics of compounds between different species .
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- HY-115761
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HDAC
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Cancer
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Dihydrochlamydocin is a histone deacetylases (HDAC) inhibitor. Dihydrochlamydocin shows strong cytostatic activity towards mastocytoma cells .
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- HY-124022
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HDAC
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Others
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HDAC-IN-69 (Compound 2) is a derivative of an HDAC inhibitor with inhibitory activity targeting maize histone deacetylase HD2 .
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- HY-117583A
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HDAC
Histone Methyltransferase
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Neurological Disease
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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. BG47 can be used for neurological disease research .
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- HY-139796
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HDAC
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Cancer
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ZYJ-34v is an orally active histone deacetylase inhibitor. ZYJ-34v has antitumor activity .
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- HY-171542
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Fungal
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Infection
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CDA-IN-2 (Compound VS#2-3) is a chitin deacetylase (Chitin Deacetylase, CDA) inhibitor with antifungal activity. At a concentration of 100 μM, it can inhibit the CDA PxCDA1 and PxCDA2 of P. xanthii by 83.7% and 74.5% respectively. CDA-IN-2 can be applied to the research in the field of controlling agricultural fungal diseases, such as dealing with resistant powdery mildew and Botrytis cinerea .
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- HY-117583
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HDAC
Histone Methyltransferase
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Neurological Disease
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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 .
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- HY-145851
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HDAC
Topoisomerase
Apoptosis
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Cancer
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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 .
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- HY-169922
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HDAC
Parasite
Caspase
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Cancer
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HDAC-IN-82 (Compound 18b) is a histone deacetylase (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 .
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- HY-105246
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Beta-lactamase
HDAC
Apoptosis
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Cancer
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Pracinostat dihydrochloride is a potent histone deacetylase (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 .
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- HY-N7036R
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- HY-W718894
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HDAC
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Others
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(R)-Dihydrolipoic acid is a compound that inhibits histone deacetylase 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.
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- HY-152235
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HDAC
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Neurological Disease
Cancer
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HDAC6-IN-15 is a selective histone deacetylase 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 .
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- HY-13322R
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SB939 (Standard)
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Beta-lactamase
HDAC
Apoptosis
Reference Standards
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Cancer
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Pracinostat (Standard) is the analytical standard of Pracinostat. This product is intended for research and analytical applications. Pracinostat is a potent histone deacetylase (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 .
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- HY-131970
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Histone Demethylase
HDAC
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Cancer
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LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
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- HY-172523
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Fungal
Parasite
Reactive Oxygen Species (ROS)
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Infection
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CDA-IN-3 (NCDI) is an inhibitor of chitin deacetylase (CDA) with anti-parasitic activity. CDA-IN-3 disrupts the chitin metabolism of nematodes, leading to an increase in the level of ROS in nematodes and causing cell damage. CDA-IN-3 has a significant inhibitory effect on all developmental stages of Caenorhabditis elegans. CDA-IN-3 can be used in the research of the anti-infection field .
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- HY-149946
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HDAC
Apoptosis
Histone Demethylase
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Cancer
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HDAC-IN-57 is an orally active inhibitor of histone deacetylases (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 .
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- HY-121315
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HDAC
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Metabolic Disease
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BRD4097 is an inhibitor of histone deacetylase (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 .
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- HY-171540
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Fungal
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Infection
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AnCDA-IN-1 (Compound J075-4187) is an inhibitor of chitin deacetylase (CDA) with antifungal activity. It has an IC50 of 4.24 μM against AnCDA of A. nidulans, a minimum inhibitory concentration (MIC) of 260 μg/mL against food spoilage fungi and plant pathogenic fungi, and a minimum fungicidal concentration (MFC) of 520 μg/mL. AnCDA-IN-1 can be used in the research of the antifungal field .
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- HY-116619
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(E/Z)-NVP-LAQ824; (E/Z)-LAQ824
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HDAC
Apoptosis
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Others
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(E/Z)-Dacinostat ((E/Z)-NVP-LAQ824) is a histone deacetylase inhibitor that has the ability to induce apoptosis and enhance the activity of fludarabine in killing leukemia cells. (E/Z)-Dacinostat can trigger the production of reactive oxygen species (ROS) and DNA damage, enhance the killing effect of fludarabine on leukemia cells, and induce apoptosis. Its mechanism is related to the regulation of DNA repair processes and intracellular signaling pathways.
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- HY-169923
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HDAC
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Cancer
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HDAC-IN-83 (compound 9D) is an inhibitor of deacetylases (HDACs) (IC50=0.01 μM/0.44 μM HDAC1/HDAC6) with anticancer, antiproliferative and caspase 3/7 activation activities. HDAC-IN-83 inhibits Cal27, HepG2 and MRC-5 with IC50s of 0.693 μM, 0.427 μM and 3.19 μM, respectively .
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- HY-144725
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HDAC
Apoptosis
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Cancer
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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 .
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- HY-130054
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|
Lysine theophyllinate
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Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
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Theophylline L-lysine (Lysine theophyllinate) is a soluble derivative of Theophylline (HY-B0809). Theophylline L-lysine is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline L-lysine inhibits PDE3 activity to relax airway smooth muscle. Theophylline L-lysine has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB into the nucleus. Theophylline L-lysine induces apoptosis. Theophylline L-lysine can be used for asthma and chronic obstructive pulmonary disease (COPD) research .
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- HY-B0809B
-
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1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate
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Endogenous Metabolite
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Cancer
|
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Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
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- HY-154855
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (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 .
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- HY-171541
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Fungal
|
Infection
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CDA-IN-1 (Compound vs#2-1) is an inhibitor of chitin deacetylase (CDA). CDA-IN-1 exhibits antifungal activity. It can inhibit fungal growth by suppressing the activity of fungal CDA, activating the plant immune response, and accumulating reactive oxygen species (ROS). At a concentration of 100 μM, CDA-IN-1 can achieve inhibition rates of 86.9% and 74.5% against PxCDA1 and PxCDA2 of P. xanthii, respectively. CDA-IN-1 can be applied to the research in the field of controlling plant fungal diseases, such as the research on diseases like cucurbit powdery mildew and tomato gray mold .
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- HY-173184
-
|
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HDAC
|
Inflammation/Immunology
|
|
HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. HDAC6-IN-53 exerts the activity of inhibiting the phenotype of idiopathic pulmonary fibrosis (IPF) by suppressing the collagen expression induced by TGF-β1, and it has demonstrated a good therapeutic effect in a mouse model of pulmonary fibrosis induced by Bleomycin (HY-17565A). HDAC6-IN-53 can be used in the research of idiopathic pulmonary fibrosis and other related pulmonary fibrosis diseases.
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- HY-161984
-
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HDAC
|
Infection
Others
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|
HDAC-IN-76 (compound 6i) is a histone deacetylase (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 .
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- HY-161778
-
|
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HDAC
VD/VDR
|
Inflammation/Immunology
Cancer
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ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (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 .
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- HY-B0809S1
-
|
1,3-Dimethylxanthine-d3; Theo-24-d3
|
Endogenous Metabolite
Adenosine Receptor
HDAC
TNF Receptor
Interleukin Related
Phosphodiesterase (PDE)
Apoptosis
Isotope-Labeled Compounds
|
Cancer
|
|
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
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- HY-139815
-
|
|
HDAC
|
Cancer
|
|
ZYJ-34c is an orally active and potent histone deacetylase 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 .
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-
- HY-176867
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|
|
HDAC
|
Neurological Disease
|
|
Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
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-
- HY-143683S
-
|
1,3-Dimethylxanthine-13C2,d6; Theo-24-13C2,d6
|
Isotope-Labeled Compounds
Phosphodiesterase (PDE)
Interleukin Related
Adenosine Receptor
Apoptosis
HDAC
TNF Receptor
Endogenous Metabolite
|
Cancer
|
|
Theophylline- 13C2,d6 (1,3-Dimethylxanthine- 13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
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-
- HY-117093
-
|
|
HDAC
|
Cancer
|
|
H8-A5 is a novel human histone deacetylase 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.
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-
- HY-136713
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|
|
Sirtuin
|
Neurological Disease
Cancer
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Sirt1/2-IN-5 is a SIRT1/SIRT2 inhibitor with human SIRT1 IC50 0.3 μM and human SIRT2 IC50 values 1.2 μM and pIC50 5.82. Sirt1/2-IN-5 inhibits NAD +-dependent deacetylase activity of SIRT1 and SIRT2. Sirt1/2-IN-5 can be used for the research of cancer, neurodegenerative disease .
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-
- HY-181768
-
|
|
Ligands for Target Protein for PROTAC
HDAC
|
Cancer
|
|
HDAC3-IN-8 is a selective inhibitor targeting HDAC1, HDAC2 and HDAC3, with IC50 values of 3.52 nM for HDAC1, 15.14 nM for HDAC2 and 0.38 nM for HDAC3. HDAC3-IN-8 shows high selectivity for HDAC3 and exerts its effect by inhibiting histone deacetylase activity. HDAC3-IN-8 can be used to construct HDAC3-targeted PROTAC degrader (HY-181767) and is suitable for the research of acute myeloid leukemia (AML) .
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- HY-111027
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|
|
Apoptosis
|
Infection
|
|
HDAC8-IN-13 is a novel histone deacetylase 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 .
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-
- HY-182061
-
|
|
Sirtuin
|
Cancer
|
|
SIRT6 activator 3 (Compound 24) is a SIRT6 activator with an EC50 of 5 μM. SIRT6 activator 3 exhibits histone deacetylation activity. SIRT6 activator 3 can be used in cancer research .
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-
- HY-180483
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 144 (Compound 3f) is a highly selective antifungal agent against Aspergillus niger, with an MIC of 7.5 μg/mL. Antifungal agent 144 simultaneously inhibits chitin deacetylase AngCDA and 1,3-β-glucan synthase. Antifungal agent 144 functions by disrupting the integrity of the fungal cell wall and does not bind to Ergosterol (HY-N0181). Antifungal agent 144 can be used for research on Aspergillus niger infections .
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-
- HY-115442
-
|
|
HDAC
Bacterial
|
Infection
Cancer
|
|
NHNB is a selective HDAC8 inhibitor (IC50 = 66.0 μM) and Peptidoglycan N-acetylglucosamine (GlcNAc) deacetylases (PGNGdacs) inhibitor. NHNB shows antibacterial and bactericidal activity against B. anthracis and B. cereus. NHNB can be used for the research of acute myeloid leukemia, Bacillus anthracis infection, and Bacillus cereus infection .
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-
- HY-P3364A
-
|
|
Fluorescent Dye
Sirtuin
HDAC
|
Others
|
|
Ac-QPKK(Ac)-AMC acetate is a p53-derived peptide conjugated with a fluorophore, which serves as a fluorescent peptide substrate for detecting the deacylase activity of zinc-dependent HDACs and sirtuins (Ex = 360 nm; Em = 460 nm) .
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-
- HY-15510S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Tenovin-6-d6 is the deuterium labeled Tenovin-6 (HY-15510). Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
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-
- HY-185554
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-102 (Compound 21) is a histone deacetylase (HDAC) inhibitor with an IC50 of 58 μM. HDAC-IN-102 inhibits total HDAC activity and exhibits partial subtype selectivity, with the R-isomer targeting HDAC2 and the S-isomer targeting HDAC8. HDAC-IN-102 exerts antioxidant effects by scavenging DPPH free radicals. HDAC-IN-102 can be used in cancer-related research .
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-
- HY-116267
-
|
|
HDAC
Apoptosis
PARP
Bcl-2 Family
Androgen Receptor
|
Cancer
|
|
MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer .
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-
- HY-182412
-
|
|
Sirtuin
|
Cancer
|
|
NH4-6 is a SIRT2 inhibitor with an IC50 of 0.032 μM against SIRT2 and an IC50 of 3 μM against SIRT1. NH4-6 inhibits the deacetylase activity of SIRT1. As a cytotoxic agent, NH4-6 reduces cancer cell viability, suppresses anchorage-independent growth of cancer cells, induces acetylation of α-tubulin, and promotes acetylation of p53. NH4-6 can be used in the research of breast cancer .
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-
- HY-181843
-
|
|
HDAC
Apoptosis
Histone Acetyltransferase
Microtubule/Tubulin
Caspase
|
Cancer
|
|
HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer .
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-
-
- HY-15149G
-
|
FK 228; FR 901228; NSC 630176
|
蛍光色素
|
|
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (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 .
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-
- HY-109521A
-
|
Manganese(Ⅱ) chloride tetrahydrate, molecular biology grade,≥99.0% (KT)
|
生化学アッセイ試薬
|
|
Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
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-
- HY-15149G
-
|
FK 228; FR 901228; NSC 630176
|
生化学アッセイ試薬
|
|
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (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 .
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-
- HY-P3364A
-
|
|
Fluorescent Dye
Sirtuin
HDAC
|
Others
|
|
Ac-QPKK(Ac)-AMC acetate is a p53-derived peptide conjugated with a fluorophore, which serves as a fluorescent peptide substrate for detecting the deacylase activity of zinc-dependent HDACs and sirtuins (Ex = 360 nm; Em = 460 nm) .
|
| 製品番号 |
製品名 |
Category |
Target |
構造式 |
-
- HY-15149S2
-
|
|
|
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (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 .
|
-
-
- HY-B0809S1
-
|
|
|
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
|
-
-
- HY-143683S
-
|
|
|
Theophylline- 13C2,d6 (1,3-Dimethylxanthine- 13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (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 .
|
-
-
- HY-15510S
-
|
|
|
Tenovin-6-d6 is the deuterium labeled Tenovin-6 (HY-15510). Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
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-
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