Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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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
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM. -
HDAC inhibitor
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts. -
HDAC6 inhibitor
Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. -
pan-HDAC inhibitor
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. -
HDAC1 and HDAC3 inhibitor
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively. -
Fluorometric HDAC Substrate
Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors. -
VUBI1 Analogue
VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
HDAC3 Inhibitor
HDAC3-IN-2 is a potent inhibitor of histone deacetylase 3 (HDAC3), with an IC50 value of 14 nM. This pyrazinyl hydrazide compound exhibits cytotoxicity against triple-negative breast cancer cell lines, demonstrating an IC50 of 0.55 μM for 4T1 cells and 0.74 μM for MDA-MB-231 cells. In in vivo studies using tumor-bearing mouse models, HDAC3-IN-2 effectively enhances histone acetylation levels at H3K9, H3K27, and H4K12 while promoting apoptosis through increased caspase-3, caspase-7, and cytochrome c levels, alongside a decrease in proliferation markers such as Bcl-2, CD44, EGFR, and Ki-67. -
HDAC1/6 Inhibitor
HDAC1/6-IN-3 is a potent inhibitor of histone deacetylases 1 and 6 (HDAC1 and HDAC6). It demonstrates strong inhibitory activity, with IC50 values of 1.1 nM for HDAC1 and 2.7 nM for HDAC6. This compound effectively induces cell cycle arrest in the G0/G1 phase and promotes both apoptosis and pyroptosis in HepG2 cells. Additionally, HDAC1/6-IN-3 exhibits significant antitumor effects in the HepG2 xenograft model and is valuable for research focused on various types of cancer, including liver, lung, colon, and breast cancers. -
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. -
HDAC Inhibitor
TH-6 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.115 µM for HDAC1, 0.135 µM for HDAC2, 0.242 µM for HDAC3, 0.138 µM for HDAC6, and 2.120 µM for HDAC8. This compound effectively inhibits cell migration and invasion while promoting apoptosis and inducing cell cycle arrest in the G2/M phase. TH-6 exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies. -
HDAC Inhibitor
HDAC-IN-36 is a potent HDAC (histone deacetylase) inhibitor that targets HDAC6 with an IC50 of 11.68 nM. This compound demonstrates significant biological activity by promoting apoptosis, enhancing autophagy, and inhibiting cellular migration. HDAC-IN-36 is applicable in cancer research, particularly in studies focusing on anti-tumor and anti-metastatic mechanisms in breast cancer. -
HDAC Inhibitor
Trichostatin C is an HDAC inhibitor that plays a crucial role in modulating gene expression by preventing the deacetylation of histones. This compound exhibits significant anticancer activity, inducing apoptosis and causing cell cycle arrest in the G2/M phase, making it particularly effective against lung cancer and urothelial bladder cancer. Additionally, Trichostatin C promotes differentiation in Friend leukemic cells and demonstrates antifungal properties, highlighting its potential in various research applications related to cancer biology and fungal infections. -
JMJD3/HDAC1/HDAC6 Inhibitor
JMJD3/HDAC-IN-1 is a dual inhibitor targeting both Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylases HDAC1 and HDAC6. With an IC50 value of 16 nM for HDAC1, this compound induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, promoting apoptosis through cleavage of caspase-7 and PARP. JMJD3/HDAC-IN-1 demonstrates significant anti-cancer activity by inhibiting cell cloning, migration, and invasion, making it valuable in cancer research and therapeutic studies. -
HDAC3/p-STAT3 Inhibitor
1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment. -
HDAC inhibitor
Nullscript is an inactive analog of Scriptaid and serves as a negative control for Scriptaid, a representative histone deacetylase (HDAC) inhibitor. Despite its inactivity as an HDAC inhibitor, Nullscript inhibits the growth of *Cryptosporidium parvum* with an IC₅₀ value of 2.1 μM.
