Catalog No.
Product Name
Application
Product Information
Citations
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HDAC1-3 PROTAC Degrader
JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications. -
HDAC Inhibitor
HDAC-IN-60 is a potent inhibitor of histone deacetylases (HDACs). This compound promotes the generation of reactive oxygen species (ROS) within cells, leading to DNA damage and subsequent activation of the mitochondrial apoptotic pathway. Additionally, HDAC-IN-60 can effectively disrupt the cell cycle at the G2/M phase, making it valuable for research in cancer biology and therapeutic interventions targeting HDACs. -
HDAC Inhibitor
MC2590 is a selective histone deacetylase (HDAC) inhibitor that targets class I and IIb HDAC isoforms, including HDAC1-3, -6, -8, and -10, with IC50 values ranging from 0.015 μM to 0.156 μM. It also inhibits other HDAC isoforms, such as HDAC4, HDAC5, HDAC7, HDAC9, and HDAC11, with higher IC50 values between 1.35 μM and 3.98 μM. MC2590 has been shown to induce G2/M cell cycle arrest and influences the expression of pro- and anti-apoptotic microRNAs, leading to the induction of apoptosis. This compound is valuable for research in cancer biology, epigenetics, and cell cycle regulation. -
HDAC/CDK Inhibitor
CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy. -
HDAC3/6 Inhibitor
HDAC3/6-IN-2 is a selective inhibitor of histone deacetylases HDAC3 and HDAC6, exhibiting IC50 values of 0.368 μM and 0.635 μM, respectively. This compound demonstrates significant antitumor activity by promoting apoptosis in cancer cells. Additionally, HDAC3/6-IN-2 reduces the levels of HDAC3 and HDAC6, leading to the upregulation of acetylated histone H3 and α-tubulin, which may enhance therapeutic outcomes for cancers associated with these targets. -
HDAC Inhibitor
HDAC-IN-71 is a potent histone deacetylase (HDAC) inhibitor that exhibits IC50 values of 12.6 nM for HDAC1, 14.1 nM for HDAC2, 20 nM for HDAC3, 3 nM for HDAC6, and 72 nM for HDAC10. This compound effectively induces apoptosis, making it a valuable tool in cancer research. Its selective inhibition of multiple HDAC isoforms can aid in elucidating the role of histone modification in tumor progression and therapeutic response. -
HDAC6 Inhibitor
C1A is an inhibitor of class I and II histone deacetylases (HDACs) as well as sirtuins, demonstrating an IC50 of 479 nM specifically for HDAC6. This compound promotes sustained acetylation of HDAC6 substrates, including α-tubulin and HSP90, contributing to its potent anticancer properties. C1A has been shown to effectively induce apoptosis in various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-2 is a potent inhibitor of lysine-specific demethylase 1 (LSD1) and several histone deacetylases (HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8), with IC50 values ranging from 1.0 to 39.0 nM. This compound demonstrates significant biological activity by inhibiting the proliferation of colorectal cancer cells, inducing apoptosis, and causing G2/M cell cycle arrest. Additionally, LSD1/HDAC-IN-2 reduces cell migration and displays antitumor efficacy in mouse models, making it a valuable tool for cancer research and therapeutic development. -
HDAC Inhibitor
HDAC-IN-42 is a potent and selective inhibitor of histone deacetylases (HDACs), displaying IC50 values of 0.19 µM for HDAC1 and 4.98 µM for HDAC6. This compound demonstrates significant anticancer and anti-proliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. HDAC-IN-42 is valuable for research applications focused on cancer biology and the modulation of gene expression through epigenetic mechanisms. -
Top/HDAC Dual Inhibitor
Top/HDAC-IN-2 is a dual inhibitor targeting topoisomerase and histone deacetylases (HDACs). This compound demonstrates significant antitumor activity and effectively induces apoptosis in cancer cells. Its ability to concurrently interfere with these critical pathways makes it a valuable tool for researchers investigating cancer therapeutics and cell death mechanisms. -
FLT3/HDAC Inhibitor
HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies. -
PROTAC HDAC6 Degrader
PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways. -
HDAC4 Inhibitor
HDAC4-IN-1 is a selective inhibitor of histone deacetylase 4 (HDAC4), demonstrating an IC50 of 0.077 μM. This compound has been shown to enhance caspase-mediated apoptosis, highlighting its potential in anticancer applications. HDAC4-IN-1 is a valuable tool for research into drug combinations aimed at increasing the efficacy of cancer therapies. -
HDAC6 Inhibitor
HDAC6-IN-45 is a selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 15.2 nM. This compound has been shown to promote neurotrophic effects by enhancing the expression of GAP43 and Beta-3 tubulin, while also activating the Nrf2 signaling pathway. Further research applications include its ability to mitigate H2O2-induced reactive oxygen species production, inhibit apoptosis in PC12 cells, and confer neuroprotective effects in SCOP-induced zebrafish models of Alzheimer's disease. Additionally, HDAC6-IN-45 exhibits antioxidant properties and possesses favorable blood-brain barrier permeability. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-2 is a potent dual inhibitor targeting topoisomerase II (Topo II) and histone deacetylases (HDAC). This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for investigating the mechanisms of tumorigenesis and potential therapeutic interventions. Research applications include studies on cancer biology, drug development, and the modulation of epigenetic regulators. -
FLT3/HDAC Inhibitor
FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies. -
HDAC Inhibitor
HDAC-IN-81 is a potent HDAC1 inhibitor, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-cancer activity by effectively inhibiting cell proliferation and inducing apoptosis in cancer cells. It serves as a valuable tool for research applications in cancer biology and epigenetic regulation. -
HDAC Inhibitor
Valproic acid magnesium is an orally active histone deacetylase (HDAC) inhibitor that exhibits an IC50 range of 0.5 to 2 mM, specifically inhibiting HDAC1 with an IC50 of 400 μM while promoting the proteasomal degradation of HDAC2. This compound activates Notch1 signaling and demonstrates anti-proliferative effects in small cell lung cancer (SCLC) cells. Valproic acid magnesium has diverse therapeutic applications, including the treatment of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and the prevention of migraine headaches. -
HDAC Inhibitor
Nanatinostat TFA is a potent, orally active inhibitor of class I histone deacetylases (HDACs), with IC50 values of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. It demonstrates reduced activity against HDAC5 and HDAC6, with IC50 values of 200 nM and 2100 nM, respectively. Nanatinostat TFA effectively induces apoptosis in myeloma cells and exhibits significant anticancer properties against various malignancies, including advanced solid tumors and colorectal cancer. Its selective inhibition of HDACs positions it as a valuable compound for cancer research and therapeutic development. -
PI3K/HDAC Inhibitor
Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways. -
HDAC Inhibitor
MC2625 is a potent histone deacetylase (HDAC) inhibitor, specifically targeting HDAC3 and HDAC6 with IC50 values of 80 nM and 11 nM, respectively. This compound effectively increases levels of acetylated histone H3 and acetylated tubulin, promoting apoptosis in cancer stem cells (CSCs) and inhibiting their growth. MC2625 serves as a valuable tool for research focused on cancer therapeutics and the role of epigenetics in tumor biology. -
HDAC Inhibitor, Topoisomerase I Inhibitor
WJ35435 is a dual-target HDAC and topoisomerase I inhibitor that exerts anticancer activity by inducing DNA damage and promoting cell cycle arrest at the G1 and G2 phases, ultimately leading to apoptosis. This compound enhances histone H3 acetylation and phosphorylation, along with α-tubulin acetylation and the formation of γ-H2AX, thereby effectively demonstrating its anti-HDAC properties. WJ35435 holds potential for advancing research in cancer therapeutics. -
HDAC Inhibitor
HDAC-IN-46 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.21 μM for HDAC1 and 0.021 μM for HDAC6. In MDA-MB-231 cells, HDAC-IN-46 promotes the upregulation of phosphorylated p38 while downregulating Bcl-xL and cyclin D1, leading to significant G2 phase cell cycle arrest and apoptosis. This compound is valuable for research focused on triple-negative breast cancer (TNBC). -
HDAC Inhibitor
HDAC-IN-57 is a potent orally active inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 2.07 nM for HDAC1, 4.71 nM for HDAC2, 2.4 nM for HDAC6, and 107 nM for HDAC8. In addition, HDAC-IN-57 inhibits lysine-specific demethylase 1 (LSD1) with an IC50 of 1.34 µM. This compound induces apoptosis and demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development targeting epigenetic regulation. -
HDAC1/HDAC2 Inhibitor
MRLB-223 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent activity against tumor cells. It induces histone hyperacetylation and activates the intrinsic apoptotic pathway, leading to tumor cell apoptosis and degradation of Bcr-Abl in a caspase-dependent manner. Notably, MRLB-223 mediates p53-independent cell death in Bcr-Abl-expressing myeloid cells and shows efficacy in animal models of Eμ-myc lymphoma. This compound is valuable for research focusing on the mechanisms of lymphomagenesis and therapeutic strategies for Eμ-myc lymphoma. -
HDAC1 Inhibitor, NTR/pH Fluorescence Inducer
HDAC-IN-101 is a selective inhibitor of HDAC1, exhibiting an IC50 of 65 nM against human HDAC1. This compound effectively inhibits cancer cell proliferation by targeting HDAC1 activity. In addition, HDAC-IN-101 is metabolically activated by overexpressed nitroreductase to produce H6AQ, which displays fluorescence under low pH conditions. Its unique properties make it valuable for applications in cancer research and cellular imaging studies. -
HCV/HDAC6 Inhibitor
Nicoxamat, also known as N-Hydroxynicotinamide, functions as an inhibitor of hepatitis C virus (HCV) and selectively targets HDAC6. This compound exhibits antiviral activity against HCV, making it a useful tool in research on hepatitis C infection. Its role as an HDAC6 inhibitor further supports investigations into epigenetic regulation and potential therapeutic strategies. -
HDAC Inhibitor
CM-444 is a potent inhibitor of histone deacetylases (HDACs) with an IC50 range of 6 nM to 0.6 μM, and demonstrates inhibition of DNA methyltransferases (DNMT) with IC50 values between 1.8 and 2.3 μM. This compound facilitates the differentiation of acute myeloid leukemia cells and exhibits significant anti-leukemic activity, enhancing survival rates in mouse models. CM-444 serves as a valuable tool for research into cancer epigenetics and the development of targeted therapies for leukemia. -
CARM1/HDAC2 inhibitor
CARM1/HDAC2-IN-1 is a dual inhibitor targeting both CARM1 and HDAC2, exhibiting IC50 values of 3.71 nM and 4.07 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. CARM1/HDAC2-IN-1 is suitable for studies investigating the role of these epigenetic regulators in tumor biology and therapeutic strategies. -
HDAC Inhibitor
HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma. -
HDAC6 Degrader
HDAC6 degrader-5 functions as an HDAC6 degrader, demonstrating potent inhibitory and degradation capabilities with an IC50 of 4.95 nM and a DC50 of 0.96 nM. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, while also preventing hepatocyte apoptosis. Additionally, HDAC6 degrader-5 shows anti-inflammatory effects in mouse models of acetaminophen-induced liver injury, making it a valuable tool for research on inflammatory diseases and liver pathologies. -
HDAC3 Degrader
HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions. -
HDAC Inhibitor
2-Propylpent-4-ynoic acid, a histone deacetylase (HDAC) inhibitor, exhibits an IC50 of 0.5 mM against human HDAC. This compound induces P-glycoprotein function and has been associated with teratogenicity, fetal growth inhibition, and neurotoxicity. Notably, the S-enantiomer demonstrates more significant teratogenic effects compared to its R-enantiomer and other analogs. 2-Propylpent-4-ynoic acid is relevant in research focused on the mechanisms underlying colon cancer and neural tube defects, including exencephaly. -
HDAC8 Modulator
LG190119 is a selective modulator of HDAC8, primarily targeting Schistosoma mansoni with reduced affinity for human HDAC8. This compound has been shown to induce apoptosis in schistosome cells, making it a valuable tool for research in anti-parasitic agents. Its ability to selectively affect parasitic cells underscores its potential in developing effective treatments against schistosomiasis. -
HDAC2 Inhibitor
HDAC2-IN-3 is a selective HDAC2 inhibitor with an IC50 of 14 nM, capable of crossing the blood-brain barrier. This compound effectively upregulates histone acetylation levels both in cultured cells and in vivo, and has been shown to enhance long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 is valuable for research applications focused on neurodegenerative disorders, particularly Alzheimer's disease. -
HDAC8 Inhibitor
HDAC8-IN-16 is a selective inhibitor of histone deacetylase 8 (HDAC8), exhibiting an IC50 of 0.16 μM. It has been shown to induce apoptosis in various cell lines, trigger G2/M phase cell cycle arrest, and moderately inhibit cancer cell proliferation. This compound is particularly relevant for research applications related to colorectal cancer, providing valuable insights into the therapeutic potential of HDAC8 modulation. -
HDAC6 Inhibitor
HDAC6-IN-78 is a highly selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 24 nM. This compound demonstrates specificity by showing no significant activity against other HDAC isoforms. HDAC6-IN-78 is valuable for research applications focused on studying the role of HDAC6 in cellular processes, including neurodegenerative diseases and cancer. -
HDAC6 Inhibitor
NCT-10b is a selective inhibitor of HDAC6, primarily targeting this enzyme to influence cellular processes. It facilitates α-tubulin acetylation while having minimal effect on histone H4 acetylation. NCT-10b is applicable in research focused on multiple myeloma, providing insights into the mechanisms of this hematological malignancy and potential therapeutic strategies. -
HDAC2 Inhiibitor
4-Phenylcinnamic acid is a weak inhibitor of HDAC2, exhibiting an IC50 value greater than 5 μM. This compound has demonstrated moderate activity in inhibiting cell growth in various tumor cell lines. Its role as an HDAC2 inhibitor makes it a useful tool for exploring the effects of histone deacetylation in cancer research and related fields.
