Catalog No.
Product Name
Application
Product Information
Citations
-
pan HDAC inhibitor
Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity. -
HDAC inhibitor
Oxamflatin (Metacept-3) is a potent HDAC inhibitor with an IC50 of 15.7 nM. -
HDAC inhibitor
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform. -
HDAC inhibitor
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. -
HDAC inhibitor
Resminostat hydrochloride is a potent inhibitor of HDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877 nM. -
HDAC Inhibitor
NCH 51 is a cell-permeable prodrug that is intracellularly converted to a potent HDAC inhibitor, with an IC50 of 48 nM. -
HDAC6 inhibitor
TCS HDAC6 20b, selective inhibitor of histone deacetylase 6 (HDAC6). Inhibits HCT116 growth in combination with taxol. Also inhibits growth of MCF-7 cells stimulated by estrogen. -
HDAC/ACE inhibitor
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. -
HDACs/mTOR Inhibitor 1
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies. -
HDAC6 inhibitor
Nexturastat A is an aryl urea derivative that acts as a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6) (IC50= 5.02 +/- 0.60 nM). -
NAD(+)-dependent histone deacetylase Sir2p inhibitor
Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 uM, showing a higher activity in a cell-based assay. -
HDAC inhibitor
Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. -
HDAC inhibitor
4SC-202 is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
-
HDAC Inhibitor
Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent. -
HDAC inhibitor
Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
HDAC inhibitor
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively. -
HDAC Inhibitor
DL-Sulforaphane N-acetyl-L-cysteine is an orally active inhibitor of histone deacetylases (HDACs) and a stable metabolite of sulforaphane. This compound enhances autophagy-mediated reduction of α-tubulin expression via the ERK signaling pathway, making it a valuable tool in cancer research. Its improved blood-brain barrier permeability and extended half-life support its potential in neurobiological studies and therapeutic applications. -
HDAC Inhibitor
Panobinostat lactate is a potent, orally active non-selective histone deacetylase (HDAC) inhibitor. It exhibits significant antineoplastic activity and has been shown to disrupt HIV latency effectively. Additionally, Panobinostat lactate induces apoptosis and autophagy in various cell types. This reagent is valuable for studying refractory or relapsed multiple myeloma and exploring HDAC inhibition in cancer research. -
PROTAC HDAC8 Degrader
SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation. -
HDAC Inhibitor
Purinostat mesylate is a selective inhibitor of histone deacetylases (HDACs), effectively targeting class I and class IIb HDACs with IC50 values ranging from 0.81 to 11.5 nM. This compound induces apoptosis and influences the cell cycle in LAMA84 and 188 BL-2 cell lines, demonstrating potent anti-leukemic effects in vivo. Purinostat mesylate serves as a valuable tool for researching lymphoblastic leukemia and its therapeutic potential. -
HDAC/JAK/BRD4 Inhibitor
HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways. -
HDAC1-3 Inhibitor
HDAC-IN-53 is a selective inhibitor of histone deacetylases 1-3, demonstrating IC50 values of 47 nM, 125 nM, and 450 nM for HDAC1, HDAC2, and HDAC3, respectively. This compound exhibits minimal off-target effects, as it does not inhibit class II HDACs (IC50 > 10 μM). HDAC-IN-53 promotes caspase-dependent apoptosis and has been shown to inhibit the growth of human tumor xenografts in nude mice, as well as murine tumors in immune-competent mice bearing MC38 colon cancer. It serves as a valuable tool for studying cancer biology and potential therapeutic strategies targeting HDAC pathways. -
HDAC6 Inhibitor
QTX125 TFA is a potent and highly selective inhibitor of Histone Deacetylase 6 (HDAC6). This compound demonstrates exceptional selectivity for HDAC6 over other isoforms, making it a valuable tool for studying the role of HDAC6 in various biological processes. QTX125 TFA has shown promising antitumor effects, indicating its potential for use in cancer research and therapeutic applications targeting HDAC6-related pathways. -
HDAC Inhibitor
CRA-026440 hydrochloride is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor, exhibiting Ki values against recombinant HDAC isoenzymes of 4 nM for HDAC1, 14 nM for HDAC2, 11 nM for HDAC3, 15 nM for HDAC6, 7 nM for HDAC8, and 20 nM for HDAC10. This compound demonstrates significant antitumor and antiangiogenic activities, making it relevant for studies in cancer biology. Additionally, CRA-026440 hydrochloride possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications for bioconjugation studies. -
HDAC1/2 and CDK2 Inhibitor
HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases. -
HDAC/MBLAC2 Inhibitor
Pracinostat dihydrochloride is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values in the range of 40-140 nM, making it a valuable tool in cancer research. In addition, it effectively inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) with an EC50 below 10 nM, highlighting its potential use in studies related to epigenetic regulation and resistance mechanisms in cancer therapies. -
HDAC Inhibitor
HDAC-IN-73 is a potent histone deacetylase (HDAC) inhibitor targeting HDAC1 and HDAC6, with IC50 values of 0.17 µM and 0.49 µM, respectively. Its enhanced activity against HDAC6 demonstrates a nine-fold greater potency compared to PsA, making it a valuable compound in the field of cancer research. HDAC-IN-73 exhibits significant antiproliferative effects, induces apoptosis, and triggers G2/M cell cycle arrest, positioning it as a promising candidate for investigating therapies in colon cancer and other malignancies. -
HDAC Inhibitor
HDAC-IN-96 is a selective inhibitor of histone deacetylases 1 and 2 (HDAC1/2), exhibiting IC50 values of 457.1 nM and 433.7 nM, respectively. This compound demonstrates significant cytotoxicity against various hematological tumor cell lines, including RS4;11, K562, RPMI-8226, and U266, with IC50 values between 2.11 and 5.35 μM. HDAC-IN-96 has been shown to induce apoptosis and cause S phase arrest in cancer cells, making it a valuable tool for research in hematological malignancies such as acute lymphoblastic leukemia. -
Aurora A/Aurora B/HDAC1/HDAC2 Inhibitor
Aurora kinase/HDAC-IN-1 is a potent dual inhibitor targeting Aurora A, Aurora B, HDAC1, and HDAC2. This compound promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis through G2/M cell-cycle arrest. It demonstrates significant antiproliferative activity in colorectal cancer cells, with an IC50 of 30.2 nM in HCT-116 cells, and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models. This reagent is valuable for research in cancer biology and therapeutic application development. -
HDAC1/CDK7 Inhibitor
HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics. -
HDAC Inhibitor
WMJ-J-09 is a potent HDAC inhibitor with sub-nanomolar activity, exhibiting IC50 values of 7.5 nM against HDAC1 and 3.9 nM against HDAC6, along with notable activity towards HDAC2, HDAC3, and HDAC8. This compound effectively disrupts the cell cycle and promotes apoptosis in cancer cells through the LKB1-AMPK-p38MAPK-p63-survivin signaling pathway. By inhibiting HDAC enzyme activity, WMJ-J-09 leads to the acetylation of critical proteins, thus contributing to the regulation of cell death in cancer models, such as HCT116 and FaDu cells.
