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Catalog No.
Product Name
Application
Product Information
Citations
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HDAC6 Inhibitor
PTG-0861 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 value of 5.92 nM. This compound effectively induces apoptosis, making it a valuable tool for research in acute myeloid leukemia, multiple myeloma, and other hematological malignancies. Its specificity towards HDAC6 positions it as a promising candidate for studies aimed at understanding epigenetic regulation in cancer. -
HDAC/ Topo II α Inhibitor
KT32 is a potent dual inhibitor targeting histone deacetylases (HDAC) and topoisomerase II alpha (Topo II α). This compound promotes cell death through the activation of apoptotic pathways, making it valuable for research in cancer biology and therapeutic studies. KT32's ability to modulate chromatin structure and DNA topology renders it an essential tool for exploring the mechanisms of tumor progression and treatment resistance. -
ATM Inhibitor
ATM Inhibitor-7 is a selective inhibitor of ataxia-telangiectasia mutated (ATM) with an IC50 of 1.0 nM. This compound effectively induces apoptosis and causes G2/M phase cell cycle arrest, particularly when combined with CPT-11. ATM Inhibitor-7 is utilized in research applications focused on elucidating mechanisms of tumor biology and enhancing the efficacy of chemotherapeutic agents. -
HDAC Inhibitor
(E/Z)-Dacinostat is a potent histone deacetylase (HDAC) inhibitor that plays a critical role in inducing apoptosis in cancer cells, particularly leukemia. By promoting the generation of reactive oxygen species (ROS) and instigating DNA damage, (E/Z)-Dacinostat enhances the cytotoxic efficacy of fludarabine against leukemia cells. Its mechanism involves modulation of DNA repair pathways and intracellular signaling, making it a valuable tool for cancer research and therapeutic investigations. -
HDAC Inhibitor
SK-7041 is a histone deacetylase (HDAC) inhibitor with an IC50 value of 172 nM. This compound promotes hyperacetylation of histones H3 and H4, leading to the inhibition of tumor cell growth both in vitro and in vivo. Additionally, SK-7041 induces apoptosis and causes cell cycle arrest at the G1 phase, making it a valuable tool for cancer research and therapeutic exploration. -
IRE1 Inhibitor
KIRA9 is a selective inhibitor of IRE1α, exhibiting an IC50 of 4.8 μM in INS-1 cells. By occupying the ATP-binding site, KIRA9 effectively disrupts endoplasmic reticulum (ER)-localized mRNA decay and inhibits apoptosis associated with ER stress. This compound serves as a valuable tool for studying the unfolded protein response and its implications in various cellular stress-related diseases. -
HDAC8 Inhibitor
HDAC8-IN-3 is a potent inhibitor of Histone Deacetylase 8 (HDAC8), exhibiting an IC50 value of 9.3 μM. This compound induces thermal stabilization and demonstrates cytotoxic effects, leading to apoptosis in leukemic cell lines. HDAC8-IN-3 is valuable for research applications focused on cancer metabolism, epigenetic regulation, and therapeutic development for hematological malignancies. -
Hsp90/HDAC6 Inhibitor
HDAC6/HSP90-IN-2 is a dual inhibitor targeting both HDAC6 and Hsp90, exhibiting IC50 values of 105.7 nM and 61 nM, respectively. This compound demonstrates significant potential in cancer research, enabling the study of mechanisms involved in tumorigenesis and the development of novel therapeutic strategies. Its ability to modulate key cellular pathways associated with cancer progression makes it a valuable tool for investigating the role of HDAC6 and Hsp90 in various malignancies. -
Wee1/HDAC Inhibitor
Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and histone deacetylases (HDACs). It demonstrates potent activity with an IC50 of 1.2 nM for Wee1 and varying IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. This compound displays significant antiproliferative effects in MV4-11 cells, with an IC50 of 0.076 μM, by disrupting DNA damage repair mechanisms and promoting apoptosis. Wee1/HDAC-IN-1 is suited for research on acute myeloid leukemia (AML). -
Topoisomerase II Inhibitor
Topoisomerase II Inhibitor 15 is a selective inhibitor of topoisomerase II, an enzyme critical for DNA replication and repair. This compound induces apoptosis and exhibits potent activity against head and neck tumors, making it a valuable tool for cancer research. Its mechanism of action further highlights its potential in studying the roles of topoisomerases in tumor biology and therapeutics. -
HDAC/DNMT Inhibitor
J208 is a dual inhibitor targeting histone deacetylase (HDAC) and DNA methyltransferase (DNMT). This compound effectively inhibits the proliferation of cancer cells and reduces the migration and invasion of triple-negative breast cancer (TNBC) cells. J208 also induces apoptosis and halts the cell cycle at the G0/G1 phase, while activating innate immune signaling pathways by promoting the expression of endogenous retroviruses (ERVs) in TNBC. It serves as a valuable tool for investigating epigenetic regulation and cancer therapy. -
ARP-1/HDAC-1 Inhibitor
DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM, respectively. This compound effectively inhibits the proliferation of various breast cancer cell lines, including MDA-MB-436, MDA-MB-231, and MCF-7, with IC50 values of 0.3, 2.7, and 2.41 μM. Additionally, DLC-50 induces apoptosis specifically in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase, making it a valuable tool for cancer research and therapeutic development. -
CDK9/HDAC Dual Inhibitor
CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models. -
HDAC1/2 Inhibitor
ZWZH-21 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, demonstrating IC50 values of 34 nM and 41 nM, respectively. This dual-action compound exhibits potent anti-proliferative effects on colorectal cancer cell lines HCT116 and SW480, with IC50 values of 0.524 μM and 1.063 μM, respectively. Additionally, ZWZH-21 effectively inhibits cell migration and prompts apoptosis in multiple colorectal cancer models, making it a valuable tool for cancer research, particularly in the study of colorectal cancer. -
Topoisomerase II Inhibitor
ICRF-196 is a racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193, functioning as a potent inhibitor of DNA Topoisomerase II. This compound effectively inhibits DNA synthesis and promotes apoptosis, exhibiting significant anti-cancer and anti-inflammatory properties. Additionally, ICRF-196 demonstrates cardioprotective effects against anthracycline-induced toxicity in cardiomyocytes. It is applicable in research focusing on cancer, infectious diseases, inflammation, and cardiovascular disorders, including acute promyelocytic leukemia. -
HDAC1/HDAC2 Inhibitor
ST13 is a selective inhibitor of HDAC1 and HDAC2, exhibiting IC50 values of 23 nM and 49 nM, respectively. It offers weak inhibition of HDAC3 and HDAC6, with IC50 values of 4.30 μM and >10 μM, respectively. The binding mechanism of ST13 involves an initial rapid formation of a collision complex followed by a slow conversion to a stable complex. This compound has demonstrated the ability to induce apoptosis in cancer cells and is useful for research on melanoma and triple-negative breast cancer. -
Topoisomerase IV Inhibitor
Ciprofloxacin lactate functions as a potent inhibitor of topoisomerase IV. It is known to induce damage to both mitochondrial and nuclear DNA, resulting in mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Additionally, ciprofloxacin lactate displays significant anti-proliferative properties and promotes apoptosis, making it valuable for various research applications in microbiology and cancer studies. This fluoroquinolone antibiotic also demonstrates strong antibacterial activity, contributing to its utility in infectious disease research. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-1 is a potent dual inhibitor targeting Topoisomerase II (Topo II) and histone deacetylases (HDACs). This compound is known to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit these targets can provide insights into novel cancer treatment strategies. -
PDE5/HDAC Inhibitor
PDE5/HDAC-IN-1 is a dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) with IC50 values of 46.3 nM and 14.5 nM, respectively. This compound has demonstrated the capability to induce cell apoptosis and exhibits significant anticancer activities. PDE5/HDAC-IN-1 is a valuable tool for research in cancer therapeutics and epigenetic modulation. -
HDAC3 Inhibitor
HDAC3-IN-6 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of 53 nM. This compound effectively induces the expression of PD-L1 in a dose-dependent manner, promoting apoptosis and elevating reactive oxygen species (ROS) production. HDAC3-IN-6 demonstrates significant antitumor efficacy, particularly in colorectal cancer models, making it a valuable tool for research into cancer therapy and immunomodulation. -
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. -
Topoisomerase Inhibitor
Topoisomerase I inhibitor 5 is a potent inhibitor that targets topoisomerase I, exhibiting an IC50 value indicative of its efficacy. This compound disrupts DNA processing and significantly inhibits topoisomerase I activity, leading to cell cycle arrest at the G1 phase and inducing apoptosis in MCF-7 cells. Additionally, Topoisomerase I inhibitor 5 demonstrates potential in reversing P-glycoprotein-mediated resistance to Adriamycin, making it a valuable tool for cancer research. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-2 is a selective inhibitor of PARP1 and BRD4, demonstrating IC50 values of 197 nM and 238 nM, respectively. This compound effectively impedes DNA damage repair mechanisms, inhibits the G0/G1 cell cycle transition, and induces apoptotic cell death. PARP1/BRD4-IN-2 has shown significant anti-tumor efficacy in the MDA-MB-468 xenograft mouse model, making it a valuable tool for research in triple-negative breast cancer (TNBC). -
DNA Topoisomerase II Inhibitor
Topoisomerase IIα-IN-4 is a non-intercalative ATP-competitive inhibitor targeting human DNA topoisomerase II. With an IC50 of 3.8 μM for TopoIIα and 10.1 μM for TopoIIβ, it effectively induces apoptosis and causes cell cycle arrest in HepG2 cells. Its potent antitumor activity against various human cancer cell lines makes Topoisomerase IIα-IN-4 a valuable reagent for cancer research and therapeutic studies. -
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. -
CDK2/Topo I Inhibitor
ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development. -
TopoisomeraseI/II Inhibitor
Erythro-Austrobailignan-6 is a selective inhibitor of DNA topoisomerase I and II, exhibiting anti-cancer properties. This compound induces apoptosis in cancer cells while also promoting the phosphorylation of p38 and JNK signaling pathways. Its ability to interfere with DNA replication makes it a valuable tool for research in cancer biology and therapeutic development. -
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. -
PARP1 Inhibitor
PARP1-IN-14 is a potent inhibitor of PARP1, displaying an IC50 of 0.6 ± 0.1 nM. It demonstrates significant antiproliferative effects on MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cell lines, with IC50 values below 0.3 nM. This compound is valuable for cancer research, particularly in studies focused on DNA repair mechanisms and therapeutic strategies for BRCA-deficient tumors. -
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. -
PARP-1 Inhibitor
PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM, targeting the PARP-1 enzyme to modulate DNA damage response pathways. It exhibits significant anti-proliferative effects in both rat (C6) and human (U87MG) glioma cell lines by promoting PARP cleavage and inducing reactive oxygen species (ROS), ultimately leading to increased cell apoptosis. Additionally, PARP1-IN-46 effectively inhibits glioma cell migration, invasion, and colony formation, making it a valuable tool for research on glioma biology and potential therapeutic strategies. -
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. -
IRE1 Inhibitor
3-Ethoxy-5,6-dibromosalicylaldehyde is a selective non-competitive inhibitor of IRE1, including IRE1α, with an IC50 of approximately 0.12 μM for human IRE1α-cyto. This compound effectively inhibits XBP-1 splicing and induces apoptosis in various cellular contexts. It has been shown to upregulate TXNIP mRNA expression while downregulating TXN expression levels. Additionally, 3-ethoxy-5,6-dibromosalicylaldehyde exhibits promising anticancer activity against pancreatic cancer and significantly inhibits the replication of chikungunya virus, making it a valuable tool for research in apoptosis and viral biology. -
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. -
DNA Topoisomerase II Inhibitor
DNA Topoisomerase II Inhibitor 1 is a potent inhibitor of DNA topoisomerase II, a crucial enzyme involved in DNA replication and maintenance. This compound exhibits significant anti-proliferative activity by inducing apoptosis and causing cell cycle arrest at the sub-G1 phase. It serves as a valuable tool for research in cancer biology and therapeutic studies targeting cell growth and survival pathways. -
PARP 2 Inhibitor
PARP-2-IN-2 is a potent inhibitor of PARP-2, exhibiting an IC50 value of 0.057 μM. This compound effectively induces cell cycle arrest and apoptosis in MCF-7 breast cancer cells, highlighting its potential as a therapeutic agent in cancer research. PARP-2-IN-2 is valuable for investigations into cancer biology and therapeutic strategies targeting DNA repair mechanisms. -
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. -
Sirtuin Inhibitor
Sirt1/2-IN-4 is a potent triple inhibitor of the sirtuin family, specifically targeting SIRT1 and SIRT2 with IC50 values of 1.2 μM and 1.9 μM, respectively, and showing moderate inhibition of SIRT3 at 18.6 μM. This compound effectively prevents the deacetylation of p53, highlighting its potential role in cancer research. Its ability to modulate sirtuin activity makes it a valuable tool for investigating the biological implications of sirtuin inhibition in various cancer models.
