Search Result
Results for "
Histone deacetylases
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-161149
-
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HDAC
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Cancer
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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 .
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-
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- HY-106409
-
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CHR-2845
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HDAC
Apoptosis
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Cancer
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Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias .
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-
-
- HY-144904
-
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HDAC
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Cancer
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MC4343 is a potent and dual inhibitor of EZH2 and histone deacetylase. MC4343 has the potential for the research of cancer disease.
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-
-
- HY-135476
-
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(-)-Depudecin
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HDAC
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Neurological Disease
Cancer
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Depudecin ((-)-Depudecin) is a histone deacetylase (HDAC) inhibitor. Depudecin can be isolated from the fungus Alternaria brassicicola .
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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-124022
-
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HDAC
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Others
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APHA Compound 8 (Compound 4) is a histone deacetylase (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 .
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-
-
- HY-120106
-
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HDAC
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Others
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BG14 is a chemical optical modulation of epigenetic regulation of transcription (COMET) probe. BG14 enables high-resolution optical control of epigenetic mechanisms using visible light and can photochromically inhibit human histone deacetylases (HDACs). BG14 can be used to study the dynamic regulation of the human genome .
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-
-
- HY-150586
-
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HDAC
Apoptosis
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Cancer
|
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PTG-0861 is a selective histone deacetylase 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 .
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-
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- HY-161984
-
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HDAC
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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-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-100384
-
NKL 22
1 Publications Verification
|
HDAC
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Neurological Disease
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NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (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 .
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-
-
- HY-13267
-
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NS 41080
|
HDAC
Apoptosis
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Cancer
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Droxinostat (NS 41080) is a histone deacetylase (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) .
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-
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- HY-120046
-
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HDAC
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Cancer
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YF479 is a potent inhibitor of histone deacetylase. 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 .
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-
-
- HY-144098
-
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Parasite
HDAC
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Others
|
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HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor, with IC50 values of 0.27 and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 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 .
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-
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- HY-152225
-
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HDAC
Apoptosis
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Cancer
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MC2625 is a potent pyridine-containing histone deacetylase (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 .
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-
-
- HY-136859
-
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HDAC
|
Cancer
|
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BATCP is a HDAC (Histone deacetylases) inhibitor .
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-
-
- HY-18362
-
|
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HDAC
|
Cancer
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HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor.
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-
-
- HY-144893
-
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HDAC
|
Cancer
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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 .
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-
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- HY-154855
-
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HDAC
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Cancer
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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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-
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- HY-100508
-
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HDAC
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Cancer
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ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation .
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-
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- HY-111048
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Corin
3 Publications Verification
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Histone Demethylase
HDAC
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Cancer
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Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
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-
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- HY-119505
-
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Others
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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-128919
-
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HDAC
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Others
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Ac-Lys-AMC (Hexanamide), also termed MAL, is a fluorescent substrate for histone deacetylase HDACs .
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- HY-143654
-
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HDAC
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Cancer
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WW437 is a histone deacetylase (HDAC) inhibitor with potent anti-breast cancer ability in vitro and in vivo.
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-
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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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-
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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-13506
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M344
2 Publications Verification
D 237; MS 344
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HDAC
|
Cancer
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M344 (D 237) is an inhibitor of histone deacetylase (IC50=100 nM) and an inducer of terminal cell fifferentiation.
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-
-
- HY-13432A
-
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CHR-3996 TFA
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HDAC
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Cancer
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Nanatinostat TFA is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM .
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-
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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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-
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- HY-13432
-
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CHR-3996
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HDAC
|
Cancer
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Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM .
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-
-
- HY-117394
-
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HDAC
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Cancer
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MD 85 is a potent histone deacetylase (HDAC) inhibitor with an EC50 of 5 μM. MD 85 can be used for cancer research .
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-
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- HY-19772
-
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ESM-HDAC391; CHR-5154; HDAC-IN-3
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HDAC
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Cancer
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GSK3117391 (ESM-HDAC391) is a histone deacetylase (HDAC) inhibitor, extracted from patent WO/2008040934 A1.
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-
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- HY-B0809S
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-
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- HY-139796
-
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HDAC
|
Cancer
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ZYJ-34v is an orally active histone deacetylase inhibitor. ZYJ-34v has antitumor activity .
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-
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- HY-118352
-
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HDAC
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Neurological Disease
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LB-205 is a pan-histone deacetylase inhibitor (HDACi). LB-205 can be used for the research of acute traumatic brain injury .
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- HY-13216
-
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HDAC
Apoptosis
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Cancer
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Pyroxamide is a potent inhibitor of histone deacetylase 1 (HDAC1) with an ID50 of 100 nM. Pyroxamide can induce apoptosis and cell cycle arrest in leukemia .
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- HY-126943
-
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HDAC
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Others
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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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- 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-100365
-
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SHP-141
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HDAC
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Cancer
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Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma .
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- HY-15489
-
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Scriptide; GCK1026
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HDAC
Autophagy
Apoptosis
Influenza Virus
|
Cancer
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Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research. Scriptaid is also a sensitizer to antivirals and has potential for epstein-barr virus (EBV)-associated lymphomas treatment.
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-
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- HY-50934
-
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N-acetyldinaline; CI-994; Goe-5549
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HDAC
Apoptosis
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Cancer
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Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
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-
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- HY-18361
-
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HDAC
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Cancer
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TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
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-
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- HY-164816
-
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HDAC
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Neurological Disease
Cancer
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FITC-SAHA is SAHA (HY-10221) conjugated with fluorescein. SAHA is an inhibitor of histone deacetylase (HDAC). FITC-SAHA can be used in cancer and Alzheimer's disease related research .
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- HY-152226
-
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HDAC
Apoptosis
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Cancer
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MC2590 is a potent pyridine-containing histone deacetylase (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 .
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-
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- HY-158308
-
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HDAC
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Cancer
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HDAC6-IN-41 (Compound E24) is a selective inhibitor for histone deacetylase 6 (HDAC6), with IC50 of 14 and 422 nM, for HDAC6 and HDAC8, respectively. HDAC6-IN-41 upregulates the acetylation of α-tubulin and histone site SMC3 .
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-
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- HY-157152
-
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HDAC
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Cancer
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HDAC-IN-65 ( compound 6) is a selective histone deacetylase (HDAC) inhibitor with IC50 value of 2.5μM. HDAC-IN-65 is a prodrug with very good bioreductive properties .
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-
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- HY-18360
-
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HDAC
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Cancer
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TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
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-
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- HY-W010835
-
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Boc-S-trityl-D-cysteine
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Amino Acid Derivatives
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Others
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Boc-D-Cys(Trt)-OH (Boc-S-trityl-D-cysteine) is an amino acid derivative with a Boc protecting group, which can be used to synthesize the bicyclic depsipeptide histone deacetylase inhibitor spirocysteine .
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- HY-145613
-
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HDAC
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Metabolic Disease
|
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5-Phenylpentan-2-one is a potent histone deacetylases (HDACs) inhibitor. 5-Phenylpentan-2-one can be used for urea cycle disorder research .
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-
-
- HY-D2280
-
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HDAC
Estrogen Receptor/ERR
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Others
|
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Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .
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-
- HY-128918
-
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HDAC
|
Cancer
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SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM. SIS17 inhibits the demyristoylation of serine hydroxymethyltransferase 2, a substrate of HDAC 11, but does not inhibit other HDACs .
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- HY-159109
-
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HDAC
|
Neurological Disease
|
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HDAC6-IN-46 (compound 12) is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 value of 6.2 nM. HDAC6-IN-46 can be used in Alzheimer's disease research .
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-
- HY-19328
-
ACY-775
2 Publications Verification
|
HDAC
|
Cardiovascular Disease
Neurological Disease
|
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ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM . ACY775 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
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-
- HY-12310
-
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DNA Methyltransferase
HDAC
|
Others
|
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RSC133 exhibits dual activity by inhibiting histone deacetylase 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 .
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- HY-163503
-
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HDAC
|
Cancer
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HDAC6-IN-38 (Compound Z-7) is an inhibitor for histone deacetylase 6 (HDAC6), with an IC50 of 3.25 nM. HDAC6-IN-38 inhibits proliferation of cells MGC‑803 .
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- HY-13906
-
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(+)-Largazole
|
Endogenous Metabolite
|
Cancer
|
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Largazole ((+)-Largazole) is a potent and selective histone deacetylase (HDAC) inhibitor with antiproliferative activity. Largazole is able to modulate gene expression and affect cell growth and differentiation. Largazole has also shown potential application value in anti-tumor suppression .
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-
- HY-N6735
-
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OSI 2040
|
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-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-13322
-
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SB939
|
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-114303
-
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Phosphodiesterase (PDE)
HDAC
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Neurological Disease
|
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CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-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 .
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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-15433
-
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JNJ-26481585
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HDAC
Apoptosis
Autophagy
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Cancer
|
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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 .
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- HY-15433A
-
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JNJ-26481585 dihydrochloride
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HDAC
Apoptosis
Autophagy
|
Cancer
|
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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 .
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- HY-156472
-
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HDAC
|
Cancer
|
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HDAC6-IN-25 (compound 8) is a selective inhibitor of HDAC6, with the IC50 of 0.6 nM .
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- HY-W339757
-
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Others
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Cancer
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Dioctanoylphosphatidic acid sodium functions as a modulator of phagocyte respiratory burst, acts as a precursor to diacylglycerol and lysophosphatidic acid, and influences the phosphorylation of the mammalian target of rapamycin (mTOR) while enhancing the viability of gallbladder carcinoma cells treated with histone deacetylase inhibitors (HDACIs); it is derived from glycerophospholipid through the action of phospholipase D.
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- HY-164539
-
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HDAC
Autophagy
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Cancer
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TMU 35435 is a histone deacetylase (HDAC) inhibitor. TMU-35435 inhibits the NHEJ pathway through ubiquitination of DNA-dependent protein kinase catalytic subunit (DNA-PKcs). In addition, TMU 35435 enhances radiosensitivity by inducing misfolded protein aggregation and autophagy in TNBC .
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- HY-117136
-
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HDAC
Caspase
Bcl-2 Family
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Cancer
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AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
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- HY-116818
-
|
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HDAC
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Neurological Disease
|
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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 .
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-
- HY-P1733
-
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BMF-Y
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Apoptosis
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Cancer
|
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BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
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-
- HY-118672
-
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|
HDAC
MMP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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HNHA is a potent histone deacetylase (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 .
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-
- HY-W718894
-
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Others
|
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-111027
-
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Apoptosis
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Infection
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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-115475
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SW-100
3 Publications Verification
|
HDAC
|
Neurological Disease
|
|
SW-100, a selective histone deacetylase 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 .
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-
- HY-126211
-
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HDAC
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Inflammation/Immunology
|
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KBH-A42 is a novel histone deacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC50 values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells .
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-
- HY-149369
-
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HDAC
Apoptosis
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Cancer
|
|
HDAC-IN-59 (compound 13a) is a potent histone deacetylase (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 .
|
-
- HY-149370
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-60 (compound 21a) is a potent histone deacetylase (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 .
|
-
- HY-161516
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-42 (compound 2b) is an HDAC6 inhibitor (IC50=0.009 μM). HDAC6-IN-42 shows significant anti-leukemia activity and synergistic effect with Decitabine (HY-A0004). HDAC6-IN-42 can be used for the AML research .
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-126566
-
|
|
Fungal
HDAC
Apoptosis
|
Infection
Cancer
|
|
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 .
|
-
- HY-163806
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
|
-
- HY-10226
-
|
R306465
|
Apoptosis
HDAC
|
Cancer
|
|
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases
the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-145815
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145816
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145818
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145819
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-145816A
-
|
|
HDAC
PROTACs
|
Cancer
|
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-149371
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC6-IN-16 (compound 5c) is a histone deacetylase 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 .
|
-
- HY-162487
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-72 (compound 7j) is the most potent HDAC1 (IC50=0.65 μM), HDAC2 (IC50=0.78 μM), HDAC3 (IC50=1.70 μM) inhibitor and antiproliferative compound. HDAC-IN-72 can be used for breast cancer research .
|
-
- HY-149859
-
|
|
HDAC
|
Neurological Disease
|
|
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 .
|
-
- HY-149372
-
|
|
HDAC
|
Cancer
|
|
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 .
|
-
- HY-161155
-
|
|
HDAC
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-163282
-
|
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- HY-100719
-
|
|
HDAC
HIV
|
Infection
Cardiovascular Disease
|
|
BRD-6929 is a?potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 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 .
|
-
- HY-149946
-
|
|
HDAC
Apoptosis
Histone Demethylase
|
Cancer
|
|
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 .
|
-
- HY-145815A
-
|
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
|
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
|
-
- HY-121315
-
|
|
HDAC
|
Metabolic Disease
|
|
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 .
|
-
- HY-139795
-
|
|
HDAC
|
Cancer
|
|
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
|
-
- HY-156094
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
|
-
- HY-15149
-
Romidepsin
Maximum Cited Publications
49 Publications Verification
FK 228; FR 901228; NSC 630176
|
HDAC
Apoptosis
|
Cancer
|
|
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-155248
-
|
|
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) .
|
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-116619
-
|
(E/Z)-NVP-LAQ824; (E/Z)-LAQ824
|
Others
|
Others
|
|
(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.
|
-
- HY-18712
-
BG45
4 Publications Verification
|
HDAC
Apoptosis
Caspase
|
Cancer
|
|
BG45 is a potent HDAC3 inhibitor with IC50 values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependent apoptosis .
|
-
- HY-115974
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-115975
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-145851
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-157436
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-30 (compound 8g) is a selective HDAC6 inhibitor with the IC50 21 nM, and increase cell protein acetylation levels .
|
-
- HY-158205
-
|
4-Hydroperoxy-2-decenoic acid ethyl ester
|
Reactive Oxygen Species
HDAC
SOD
|
Inflammation/Immunology
Cancer
|
|
HPO-DAEE (4-Hydroperoxy-2-decenoic acid ethyl ester) elicits nuclear accumulation of Nrf2 and activated antioxidant response element (ARE). HPO-DAEE induces antioxidant genes upregulation (eg: HO-1) through Nrf2-ARE signaling. HPO-DAEE induces reactive oxygen species generation. HPO-DAEE also inhibits histone deacetylase and upregulate expression of extracellular superoxide dismutase via histone acetylation. HPO-DAEE protects against 6-hydroxydopamine-induced cell death via activation of Nrf2-ARE and eIF2α-ATF4 pathways .
|
-
- HY-163535
-
|
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
|
-
- HY-152173
-
|
|
HDAC
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
HDAC-IN-51 is a potent histone deacetylase (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 .
|
-
- HY-119939
-
|
|
HDAC
|
Cancer
|
|
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (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 .
|
-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (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 .
|
-
- HY-146750
-
|
|
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 .
|
-
- HY-117374
-
|
|
HDAC
|
Cancer
|
|
HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM .
|
-
- HY-150503
-
|
|
HDAC
|
Neurological Disease
|
|
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 .
|
-
- HY-157385
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-107909
-
|
1,3-Dimethylxanthine sodium glycinate; Theo-24 sodium glycinate
|
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Cancer
|
|
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 .
|
-
- HY-123295
-
|
|
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 .
|
-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (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 .
|
-
- HY-169075
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-161778
-
|
|
HDAC
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-151364
-
|
|
HDAC
|
Cancer
|
|
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 .
|
-
- HY-B0809
-
|
1,3-Dimethylxanthine; Theo-24
|
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
Endogenous Metabolite
|
Cancer
|
|
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-B0809B
-
|
1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
|
Cancer
|
|
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 .
|
-
- HY-B0809A
-
|
1,3-Dimethylxanthine monohydrate; Theo-24 monohydrate
|
Phosphodiesterase (PDE)
Adenosine Receptor
HDAC
Apoptosis
Interleukin Related
TNF Receptor
Endogenous Metabolite
|
Cancer
|
|
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 .
|
-
- 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 .
|
-
- HY-146351
-
|
|
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) .
|
-
- HY-146392
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-146678
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
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 .
|
-
- HY-146679
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
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 .
|
-
- HY-149418
-
|
|
HDAC
Cholinesterase (ChE)
Tau Protein
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Neurological Disease
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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.
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- HY-B0809R
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1,3-Dimethylxanthine(Standard); Theo-24 (Standard)
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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-B0809S1
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1,3-Dimethylxanthine-d3; Theo-24-d3
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Endogenous Metabolite
Adenosine Receptor
HDAC
TNF Receptor
Interleukin Related
Phosphodiesterase (PDE)
Apoptosis
Isotope-Labeled Compounds
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Cancer
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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-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-117093
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Others
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Cancer
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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-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-146293
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HDAC
HSP
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Cancer
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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 .
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- HY-135115
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3,4-DHPEA-EA
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Others
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Inflammation/Immunology
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Oleuropein aglycone is a polyphenol and an aglycone form of Oleuropein (HY-N0292) that has been found in extra virgin olive oil and has diverse biological activities. It is formed from oleuropein via enzymatic, acidic, or acetyl hydrolysis. Dietary administration of oleuropein aglycone (50 mg/kg of food) increases the number of neuronal autophagic vesicles and reverses cognitive deficits in a TgCRND8 transgenic mouse model of Alzheimer’s disease. It also decreases cortical and hippocampal levels of histone deacetylase 2 (HDAC2) and restores long-term potentiation in the same model. Oleuropein aglycone increases urinary norepinephrine, as well as interscapular brown adipose tissue epinephrine and UCP1 protein levels, and decreases plasma leptin levels and total abdominal cavity adipose tissue weight in a rat model of high-fat diet-induced obesity. It also reduces lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
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- HY-144782
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HDAC
Autophagy
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Cancer
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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 .
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- HY-144779
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HDAC
Autophagy
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Cancer
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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 .
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- HY-144782A
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HDAC
Autophagy
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Cancer
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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 .
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- HY-144694
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HSP
HDAC
Fungal
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Infection
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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 .
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| Cat. No. |
Product Name |
Type |
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- HY-D2280
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Fluorescent Dyes/Probes
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Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .
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Product Name |
Target |
Research Area |
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- HY-W010835
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Boc-S-trityl-D-cysteine
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Amino Acid Derivatives
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Others
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Boc-D-Cys(Trt)-OH (Boc-S-trityl-D-cysteine) is an amino acid derivative with a Boc protecting group, which can be used to synthesize the bicyclic depsipeptide histone deacetylase inhibitor spirocysteine .
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- HY-P1733
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BMF-Y
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Apoptosis
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Cancer
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BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0809S
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Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
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- HY-B0809S1
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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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| Cat. No. |
Product Name |
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Classification |
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- HY-126943
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Alkynes
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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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