Catalog No.
Product Name
Application
Product Information
Citations
-
PARP Inhibitor
Schisandronic acid is a potent PARP inhibitor derived from the triterpenoid compound found in Schisandra chinensis. This compound exhibits significant cytotoxicity against human breast cancer cells, particularly MCF-7, with an IC50 value of 8.06 μM. Schisandronic acid effectively induces apoptosis through the upregulation of active caspase-3 and cleavage of PARP, while also reducing reactive oxygen species generation, thereby demonstrating notable antioxidant properties. Its mechanisms of action make Schisandronic acid a valuable tool for cancer research and therapeutic investigations. -
Topoisomerase II Inhibitor
Topoisomerase IIα-IN-5 is an inhibitor of topoisomerase IIα, effectively interfering with its catalytic activity. It operates by intercalating into DNA and binding to the minor groove, thereby inhibiting the enzyme's function. This compound demonstrates enhanced efficacy and reduced genotoxicity compared to Etoposide, making it a valuable tool for research applications focused on cancer therapy and DNA topology modulation. -
eIF4A Inhibitor
MG-002 is a selective eIF4A inhibitor that interferes with the recruitment and scanning of ribosomes by non-productively trapping the eukaryotic translation initiation factor 4A (eIF4A) onto RNA. This action effectively inhibits mRNA translation, leading to reduced growth and metastasis of triple-negative breast cancer (TNBC) tumors, as well as inducing apoptosis in cancer cells. Additionally, MG-002 significantly downregulates the protein expression of c-MYC and cyclin D1, making it a valuable tool for research applications focused on TNBC and other related malignancies. -
SIRT2 Inhibitor
SIRT2-IN-18 is a selective SIRT2 inhibitor, exhibiting IC50 values of 5.3 μM for SmSIRT2 and 12.3 μM for hSIRT2. This compound demonstrates significant antischistosomal effects against both Liberian and Puerto Rican strains of Schistosoma mansoni, effectively reducing schistosomula viability, adult worm pairing, and egg production while maintaining low cytotoxicity in mammalian cells. SIRT2-IN-18 also promotes histone H3 hyperacetylation and triggers cytochrome c-mediated apoptosis, making it a valuable tool for research into both parasitic infections and the modulation of acetylation pathways. -
Nucleoside Analog
CNDAC is a nucleoside analog that functions as a metabolite of the orally active agent Sapacitabine. It effectively induces DNA damage and promotes apoptosis in target cells. This compound is primarily utilized in research applications focused on studying cancer biology, particularly in understanding the mechanisms of DNA repair and the therapeutic potential of nucleoside analogs in cancer treatment. -
HDAC Inhibitor
HDAC-IN-39 is a potent inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 1.07 μM for HDAC1, 1.47 μM for HDAC2, and 2.27 μM for HDAC3. This compound also significantly disrupts microtubule polymerization and induces cell cycle arrest at the G2/M phase, highlighting its potential for modulating cell cycle dynamics. Furthermore, HDAC-IN-39 demonstrates promising anticancer activity, particularly against resistant cancer cell lines, making it a valuable tool for cancer research and therapeutic exploration. -
DNA Alkylator
Seco-Duocarmycin SA is a potent DNA alkylator that functions as an antitumor antibiotic with an IC50 of 10 pM. It induces a concentration-dependent increase in apoptotic cell death and is known to cause significant cell cycle arrest in the S and G2/M phases. Additionally, Seco-Duocarmycin SA acts as a cytotoxic agent in antibody-drug conjugates (ADCs), making it a valuable tool for cancer research and therapeutic development. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-3 is an orally active dual inhibitor targeting topoisomerase and histone deacetylase (HDAC). This compound enhances intracellular levels of reactive oxygen species (ROS), leading to DNA damage and subsequently inhibiting cancer cell colony formation and migration. Additionally, Top/HDAC-IN-3 induces apoptosis and cell cycle arrest in cancer cells. In non-small cell lung cancer (NSCLC) models, it demonstrates significant antitumor activity, achieving a tumor growth inhibition (TGI) of 77.5% at a dosage of 100 mg/kg. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-1 is a selective inhibitor targeting both PARP1 and BRD4, demonstrating IC50 values of 49 nM and 202 nM, respectively. This compound effectively represses the expression and activity of these proteins, leading to synergistic inhibition of malignant pancreatic cancer cell growth. PARP1/BRD4-IN-1 is a valuable tool for exploring therapeutic strategies in cancer research, particularly in the context of PARP and BRD4 signaling pathways. -
Topoisomerase I/II Inhibitor
Topoisomerase I/II Inhibitor 4 is a potent dual inhibitor targeting both topoisomerase I and II. This compound exhibits significant anti-proliferative effects, inhibiting cell growth, invasion, and migration while promoting apoptosis in cancer cells. Its primary research applications include studies focused on liver cancer therapeutics and the exploration of topoisomerase-related mechanisms in cellular processes. -
HDAC6 Inhibitor
TNI-97 is a highly selective and orally active inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.2 nM. This compound effectively suppresses the growth and clonogenicity of triple-negative breast cancer (TNBC) cells, specifically MDA-MB-453. TNI-97 induces PANoptosis, encompassing apoptosis, necroptosis, and pyroptosis in these cells. Additionally, TNI-97 demonstrates significant antitumor activity in mouse models, including xenografts and allografts of TNBC, making it a valuable tool for research focused on triple-negative breast cancer. -
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. -
Purine Nucleoside Analog
5'-Deoxy-5'-iodothymidine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its mechanism of action involves the inhibition of DNA synthesis and the induction of apoptosis in cancer cells, making it a valuable tool for cancer research. This compound is utilized in studies aiming to explore novel therapeutic approaches for lymphoid malignancies. -
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. -
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.
