Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
DNA Alkylator
Illudin M is a cytotoxic fungal sesquiterpene that functions as a DNA alkylator. Derived from the culture medium of Omphalotus illudens mushrooms, Illudin M exhibits significant anti-tumor properties. Its ability to alkylate DNA positions it as a valuable tool for research into cancer therapeutics and mechanisms of DNA damage response. -
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. -
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. -
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. -
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. -
PARP1 Inhibitor
KU-0058948 hydrochloride is a highly selective inhibitor of PARP1, exhibiting an IC50 of 3.4 nM. It is demonstrated to induce cell cycle arrest and apoptosis in primary myeloid leukemic cells and various myeloid leukemic cell lines. This reagent is valuable for research into the mechanisms of leukemia and the therapeutic potential of PARP inhibition in hematological malignancies. -
Topoisomerase II Inhibitor
Topoisomerase II inhibitor 10 is a potent inhibitor of the topoisomerase II enzyme, exhibiting an IC50 value of 7.45 µM. This compound effectively induces cell cycle arrest in the G2-M phase and promotes apoptosis in HepG-2 cells. Additionally, Topoisomerase II inhibitor 10 demonstrates significant anti-proliferative activity against various cancer cell lines, including HepG-2, MCF-7, and HCT-116, making it a valuable tool for cancer research applications. -
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). -
PARP1/NAMPT Inhibitor
PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research 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. -
PARP1/c-Met Inhibitor
PARP1/c-Met-IN-1 is a selective dual inhibitor targeting PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest in the G2/M phase in MDA-MB-231 cells. Additionally, PARP1/c-Met-IN-1 has shown significant antitumor activity in murine models, making it a valuable tool for cancer research and therapeutic development. -
PARP1 Inhibitor
PARP1-IN-10 is a potent inhibitor of PARP1, exhibiting an IC50 value of 50.62 nM in vitro without inducing cytotoxic effects. This compound induces cell cycle arrest at the G2/M phase and promotes apoptosis, thereby enhancing the cytotoxic efficacy of temozolomide (TMZ). PARP1-IN-10 is valuable for research in cancer biology and therapeutics, particularly in understanding the interplay between DNA repair mechanisms and chemotherapeutic sensitivity. -
PARP1 Inhibitor
PARP1-IN-55 is a selective inhibitor of PARP1, demonstrating potent activity with an IC50 of 0.019 μM. It exhibits considerable anti-proliferative effects on MCF-7 breast cancer cells, with an IC50 of 3.6 μM. By inhibiting the PARP1-mediated DNA damage repair pathway, PARP1-IN-55 induces reactive oxygen species accumulation, disrupts mitochondrial membrane potential, and promotes apoptosis while inhibiting cancer cell migration, invasion, and colony formation. This compound serves as a valuable tool for investigating breast cancer biology and therapeutic strategies. -
Purine Nucleoside Analog
TLR7 Agonist 9 is a purine nucleoside analog that specifically activates Toll-like receptor 7 (TLR7). This compound demonstrates immunostimulatory properties, making it suitable for research in cancer and infectious disease. Additionally, TLR7 Agonist 9 features an alkyne group, facilitating its use in click chemistry for the copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
ATM Inhibitor
Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit the growth of various hematopoietic cell lines. Furthermore, in combination with the ATR inhibitor Tuvusertib, Lartesertib enhances tumor cell apoptosis and activates immune signaling pathways, showcasing significant anti-tumor efficacy. -
ATM Inhibitor
(Rac)-Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit cell proliferation in various hematopoietic cell lines. Moreover, when used in conjunction with the ATR inhibitor Tuvusertib, (Rac)-Lartesertib can enhance tumor cell death, activate immune signaling pathways, and exhibit notable anti-tumor efficacy, making it a valuable tool for cancer research. -
SIRT6 Activator
MDL-811 is a selective allosteric activator of SIRT6, exhibiting an EC50 of 5.7 μM. This compound demonstrates significant anti-inflammatory, antitumor, and neuroprotective properties, making it a valuable tool for research. MDL-811 is particularly relevant for studies related to colorectal cancer and ischemic stroke, providing insights into potential therapeutic strategies targeting SIRT6 modulation. -
Topoisomerase I Inhibitor
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I, a key enzyme involved in DNA replication and repair. This compound disrupts the enzyme's catalytic activity, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. Topoisomerase I inhibitor 11 is primarily utilized in cancer research, particularly for studying mechanisms of drug resistance and the therapeutic potential of targeting Topoisomerase I in various malignancies.
