Catalog No.
Product Name
Application
Product Information
Citations
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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. -
DNA Synthesis Inhibitor
(rel)-Oxaliplatin is a DNA synthesis inhibitor that functions through the formation of DNA crosslinks, thereby obstructing DNA replication and transcription. This compound induces apoptosis in cancer cells, making it a valuable tool for studying cancer biology and treatment mechanisms. It is widely utilized in cancer research to explore therapeutic strategies targeting DNA repair pathways. -
Purine Nucleoside Analog
2'-O-Methyl-5-iodouridine 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, making it a valuable tool in cancer research. This compound can be utilized in studies aimed at understanding the biochemical pathways of cancer and the development of novel therapeutic strategies. -
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. -
Topoisomerase Inhibitor
Cholesteryl hemisuccinate is a topoisomerase inhibitor with notable hepatoprotective and anticancer properties. It effectively mitigates acetaminophen-induced hepatotoxicity by preventing hepatic apoptosis and necrosis. Additionally, cholesteryl hemisuccinate interferes with DNA replication and repair mechanisms by inhibiting DNA polymerase and DNA topoisomerase, ultimately leading to reduced tumor growth. This compound is suitable for applications in cancer research and liver protection studies. -
Topoisomerase II Inhibitor
Etoposide phosphate is a selective inhibitor of topoisomerase II, instrumental in disrupting DNA re-ligation processes. As the phosphate ester proagent of etoposide, it exhibits potent anti-cancer activity by inducing cell cycle arrest, apoptosis, and autophagy in cancer cells. This compound is primarily employed in cancer research to explore mechanisms of action and potential therapeutic strategies in oncology. -
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. -
SIRT7 Inhibitor
SIRT7 Inhibitor 97491 is a selective inhibitor of the SIRT7 enzyme, exhibiting an IC50 of 325 nM and effectively reducing its deacetylase activity in a dose-dependent manner. This compound enhances tumor suppression by stabilizing the p53 protein through acetylation at lysine residues K373 and K382. Additionally, SIRT7 Inhibitor 97491 promotes apoptosis via the caspase signaling pathway, making it a valuable tool for cancer research and studies focused on elucidating the role of SIRT7 in tumor progression. -
eIF4A Inhibitor
CR-1-31-B is a synthetic rocaglate that serves as a potent inhibitor of the eukaryotic translation initiation factor eIF4A. By disrupting the interaction between eIF4A and RNA, CR-1-31-B impedes the initiation phase of protein synthesis. This compound has been shown to affect the association of Plasmodium falciparum eIF4A with RNA and induce apoptosis in neuroblastoma and gallbladder cancer cells, making it a valuable tool for studying mechanisms of protein synthesis and cancer biology. -
Topoisomerase II Inhibitor
ICRF-193 is a potent inhibitor of DNA Topoisomerase II, disrupting DNA synthesis and inducing apoptosis in cancer cells. This compound exhibits significant anti-cancer and anti-inflammatory activities, making it valuable for research in oncology and inflammation. Additionally, ICRF-193 demonstrates cardioprotective properties against anthracycline-induced toxicity in cardiomyocytes. It is particularly relevant for studies focusing on acute promyelocytic leukemia, as well as broader investigations into cancer, infection, inflammation, and cardiovascular conditions. -
Fluorescent Tag
Ethidium bromide is a fluorescent intercalating agent widely used in molecular biology as a nucleic acid stain. It inserts between DNA base pairs, allowing visualization of DNA and RNA under ultraviolet (UV) light during techniques such as agarose gel electrophoresis. Due to its high sensitivity and strong fluorescence, Ethidium bromide is a standard tool for nucleic acid detection, though it is handled with caution because of its mutagenic properties. -
RNA Aptamers Probe
DFHBI-1T is a membrane-permeable fluorescent probe activated by RNA aptamers, with excitation/emission maxima at 472/507 nm. It specifically binds to aptamers such as Spinach, Spinach2, iSpinach, and Broccoli, resulting in bright fluorescence with low background signal. DFHBI-1T is commonly used for live-cell imaging of RNA. -
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. -
HDAC6-UBD antagonist
SGC-UBD253 is a potent antagonist of the HDAC6 ubiquitin-binding domain (UBD). It is suitable for use in cancer research. -
HDAC1/DNA Methyltransferase Inhibitor
Psammaplin A, a marine-derived metabolite, is a potent inhibitor of HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM), and aminopeptidase N (IC50: 18 μM). It also suppresses DNA topoisomerase and farnesyl protein transferase activities. As a PPARγ activator, Psammaplin A induces apoptosis and exhibits antitumor, anti-inflammatory, and anti-angiogenic properties. Additionally, it demonstrates antibacterial activity against Gram-positive bacteria by inhibiting DNA synthesis and DNA -
SAHH inhibitor
Adenosine dialdehyde is a purine nucleoside analogue and a potent inhibitor of S-adenosylhomocysteine hydrolase (SAHH), with a Ki of 3.3 nM. By inhibiting SAHH, it disrupts methylation-dependent processes, contributing to its demonstrated anti-tumor activity in vivo. Adenosine dialdehyde is a valuable tool in cancer research, particularly in studies targeting epigenetic regulation and methylation pathways. -
DNA polymerase theta (Polθ) inhibitor
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ), with an IC50 of 5.8 nM as measured by the PicoGreen assay. It exhibits significant antitumor efficacy in mouse xenograft models. Additionally, RP-6685 contains an alkyne functional group, making it a useful click chemistry reagent capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, enabling its application in chemical biology and drug discovery research. -
DHX9 inhibitor
ATX968 (example 31) is an orally active, potent, and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 of 0.054 μM in circBRIP1-expressing models. It demonstrates robust and durable tumor growth inhibition or regression in mouse xenograft studies using microsatellite instability-high (MSI-H) and mismatch repair-deficient (dMMR) colorectal cancer cell lines, highlighting its potential for targeted cancer therapy. - L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
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Polθ DNA polymerase inhibitor
ART899 is a highly specific allosteric inhibitor of the DNA polymerase domain of polymerase theta (Polθ). It effectively enhances the radiosensitivity of tumor cells and demonstrates good tolerability when combined with fractionated radiation therapy. ART899 significantly reduces tumor growth compared to radiation alone, making it a promising candidate for combination cancer radiotherapy strategies. -
DNA Alkylator
Illudin S is a natural sesquiterpene compound with potent cytotoxic, anti-tumor, and antiviral activities. It exhibits genotoxic effects and disrupts cell cycle progression by blocking the G1-S phase transition in human leukemia cells. Illudin S is of interest in cancer research due to its ability to target rapidly proliferating cells. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
PARG inhibitor
COH34 is a potent and selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG), with an IC50 of 0.37 nM. It binds to the catalytic domain of PARG (Kd = 0.547 μM), prolonging PARylation at sites of DNA damage and trapping DNA repair factors, thereby interfering with the DNA damage response. -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
DNA polymerase inhibitor
Aphidicolin is a tetracyclic diterpenoid antibiotic produced by the mold Cephalosporium aphidicola, known for its potent and selective inhibition of DNA polymerase α and δ. By interfering with these polymerases, Aphidicolin blocks DNA synthesis and prevents mitotic cell division, making it a valuable tool for studying cell cycle regulation and DNA replication. In addition to its antiproliferative properties, Aphidicolin inhibits viral DNA synthesis and demonstrates antiviral activity against herpes simplex virus and orthopoxviruses. It also enhances apoptosis induced by arabinosyl nucleosides in human promyelocytic leukemia cells, suggesting potential in combination therapies for cancer and viral infections. Aphidicolin is widely used in research involving DNA replication stress, antiviral mechanisms, and cell cycle synchronization. -
POLRMT inhibitor
IMT1 is a first-in-class, specific, and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). It induces a conformational change in POLRMT, preventing substrate binding and inhibiting transcription in a dose-dependent manner in vitro. IMT1 decreases deoxynucleoside triphosphate levels and citric acid cycle intermediates, leading to significant depletion of cellular amino acid levels. IMT1 holds potential for the treatment of diseases associated with mitochondrial transcription disorders. -
DNA Repair/Replicase Modulator
N-Nitrosodiethylamine (Diethylnitrosamine, DEN) is a highly potent hepatocarcinogenic dialkylnitrosamine found in tobacco smoke, water, cheddar cheese, cured and fried foods, and various alcoholic beverages. It induces alterations in nuclear enzymes involved in DNA repair and replication, contributing to its carcinogenicity. DEN causes tumors across multiple animal species, primarily affecting the nasal cavity, trachea, lung, esophagus, and liver. -
WRN inhibitor
HRO761 (Werner syndrome RecQ helicase-IN-1, example 42) is a potent and selective inhibitor of the Werner syndrome RecQ DNA helicase (WRN), an essential enzyme involved in DNA replication, repair, and genome stability. Inhibition of WRN has shown synthetic lethality in cancers with microsatellite instability (MSI) or deficient DNA mismatch repair (dMMR), making HRO761 a promising candidate for targeted cancer therapy. It is being explored in preclinical cancer research to evaluate its efficacy in selectively killing WRN-dependent tumor cells while sparing normal cells. -
PolΘ inhibitor
PolQi2 is a selective inhibitor of DNA polymerase theta (Polθ), specifically targeting its N-terminal helicase domain to suppress the alternative end-joining (alt-EJ) DNA repair pathway. By inhibiting Polθ, PolQi2 enhances the precision and integration efficiency of CRISPR/Cas9-mediated gene editing across diverse genomic loci and cell lines. Furthermore, when used in combination with DNA-PK inhibitors, PolQi2 significantly reduces off-target effects associated with Cas9 activity. These properties make PolQi2 a valuable tool for improving the fidelity and efficiency of gene editing applications in both basic research and potential therapeutic contexts. -
RNA pol III inhibitor
ML-60218 is a broad-spectrum RNA polymerase III (Pol III) inhibitor with IC₅₀ values of 32 μM in *Saccharomyces cerevisiae* and 27 μM in human cells. It inhibits Pol III–mediated transcription, which is essential for the synthesis of small RNAs such as tRNAs and 5S rRNA. ML-60218 has been shown to disrupt pre-assembled viroplasms and prevent the formation of new ones, indicating its antiviral potential. Notably, this activity occurs independently of de novo transcription of host cellular RNAs, suggesting a direct effect on viral replication machinery. ML-60218 is a valuable tool for studying Pol III function and holds potential for antiviral research. -
POLRMT inhibitor
IMT1B (LDC203974) is an orally bioavailable, noncompetitive, and selective allosteric inhibitor of mitochondrial RNA polymerase (POLRMT). By targeting POLRMT, IMT1B disrupts mitochondrial DNA (mtDNA) transcription and impairs mitochondrial gene expression, leading to reduced mitochondrial function. This mechanism contributes to its potent anti-tumor effects, particularly in cancer cells that are highly dependent on mitochondrial metabolism. IMT1B holds promise as a therapeutic agent for targeting mitochondrial vulnerabilities in tumors. -
glutamine amidotransferase inhibitor
Azaserine (CI-337) is a glutamine analog and competitive inhibitor of glutamine amidotransferase, an enzyme involved in nucleotide biosynthesis. It exhibits both antibiotic and antitumor properties by disrupting glutamine-dependent metabolic processes essential for cell proliferation. Azaserine demonstrates antibacterial activity and has shown antitumor effects in various cancer models. However, it has also been reported to possess tumorigenic potential under certain conditions, warranting cautious evaluation. -
HDAC11 inhibitor
Elevenostat (JB3-22) is a selective histone deacetylase 11 (HDAC11) inhibitor with an IC₅₀ of 0.235 µM. It exhibits antitumor activity by inducing apoptosis in multiple myeloma cells and shows potential as a therapeutic agent in hematologic malignancies. Additionally, Elevenostat has been shown to inhibit the maturation of mouse oocytes, suggesting a role for HDAC11 in reproductive biology and offering a tool for studying epigenetic regulation in oocyte development. -
HDAC6/HDAC10/LTA4H Inhibitor
Bufexamac is a nonsteroidal anti-inflammatory drug (NSAID) that functions as a dual inhibitor of class IIb histone deacetylases—HDAC6 and HDAC10—as well as leukotriene A4 hydrolase (LTA4H). It exhibits binding affinities (K\_d) of 0.53 µM for HDAC6 and 0.22 µM for HDAC10. Through its dual inhibitory activity, Bufexamac combines epigenetic modulation with anti-inflammatory effects, making it a valuable compound for research in inflammation, immune regulation, and HDAC-related pathologies. -
HDAC6 inhibitor
TYA-018 is an orally active, potent, and highly selective inhibitor of histone deacetylase 6 (HDAC6). In preclinical studies, TYA-018 demonstrates cardioprotective effects by preserving heart function in mice. Additionally, it enhances systemic energetics by upregulating the expression of genes involved in fatty acid metabolism, protein turnover, and oxidative phosphorylation, highlighting its potential in both cardiovascular and metabolic disease research. -
Snail/HDAC inhibitor
CYD19 is a potent dual-target inhibitor that simultaneously disrupts Snail and HDAC1 activity. It exhibits an IC₅₀ of 0.405 μM against HDAC1 and binds Snail with a K\_d of 0.18 μM. In HCT-116 colorectal cancer cells, CYD19 increases histone H4 acetylation and downregulates Snail protein expression, leading to the induction of apoptosis. This dual mechanism positions CYD19 as a promising therapeutic candidate for targeting epithelial–mesenchymal transition (EMT) and epigenetic dysregulation in cancer. -
CoreDAC Inhibitor
TNG260 is a selective and orally bioavailable inhibitor of histone deacetylase 1 (HDAC1) and the CoREST transcriptional corepressor complex. It exhibits approximately 10-fold selectivity for HDAC1 over HDAC3 and 500-fold selectivity for the CoREST complex compared to other HDAC-containing complexes such as NuRD and Sin3. TNG260 modulates the tumor immune microenvironment by reducing immunosuppressive neutrophil infiltration, enhancing effector T cell recruitment, and reversing anti-PD-1 resistance associated with STK11 mutations through inhibition of the CoREST–HDAC1 axis. In preclinical models, TNG260 induces durable tumor regression when combined with α-PD-1 therapy in MC38 tumor-bearing mice harboring STK11 mutations, while demonstrating reduced hematologic toxicity compared to non-selective HDAC inhibitors. -
phospholipase A2/HDAC2 inhibitor
Rhamnetin is a naturally occurring flavonoid and quercetin derivative found in *Coriandrum sativum*. It functions as an inhibitor of secretory phospholipase A₂ and histone deacetylase 2 (HDAC2), contributing to its broad pharmacological profile. Rhamnetin exhibits notable antitumor, antioxidant, and anti-inflammatory activities, making it a promising compound for research in cancer, oxidative stress-related conditions, and inflammatory diseases. -
HDAC10 inhibitor
DKFZ-748 is a selective histone deacetylase 10 (HDAC10) inhibitor with a pIC₅₀ of 7.66, corresponding to an IC₅₀ of approximately 22 nM. It exhibits antitumor activity, making it a valuable tool for studying HDAC10-mediated biological processes and a promising candidate for the development of targeted cancer therapies. -
HDAC6 inhibitor
KA2507 is a potent, orally active, and highly selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 2.5 nM. It exhibits strong antitumor activity and immunomodulatory effects in preclinical models, making it a promising candidate for cancer therapy, particularly in tumors where HDAC6 plays a key role in tumor progression and immune evasion. -
GRK5 inhibitor
KR-39038 is a potent and orally bioavailable inhibitor of G protein-coupled receptor kinase 5 (GRK5), with an IC₅₀ of 0.02 μM. It effectively suppresses angiotensin II–induced cellular hypertrophy by inhibiting the HDAC5 signaling pathway in neonatal cardiomyocytes. KR-39038 exhibits strong anti-hypertrophic activity and improves cardiac function in preclinical models, making it a promising candidate for research in heart failure and related cardiovascular diseases. -
HDAC6 inhibitor
T-518 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 36 nM for human HDAC6. It is capable of crossing the blood–brain barrier, making it suitable for central nervous system applications. T-518 is particularly useful in tauopathy research, where HDAC6 inhibition may modulate tau pathology and neurodegenerative processes. -
HDAC1 inhibitor
9-Hydroxyoctadecanoic acid (9-HSA) is a naturally derived inhibitor of histone deacetylase 1 (HDAC1), inhibiting approximately 66.4% of HDAC1 enzymatic activity at a concentration of 5 μM. It exhibits notable anticancer activity, likely through epigenetic modulation of gene expression, making it a promising compound for cancer research and therapeutic development targeting HDAC1-regulated pathways. -
HDAC6 inhibitor
SE-7552 is an orally active, highly selective histone deacetylase 6 (HDAC6) inhibitor, based on a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) scaffold, with an IC₅₀ of 33 nM. As a non-hydroxamate HDAC6 inhibitor, SE-7552 demonstrates exceptional isoform selectivity, showing over 850-fold preference for HDAC6 compared to other HDAC isozymes. In preclinical studies, SE-7552 effectively inhibits multiple myeloma tumor growth in vivo and also exhibits anti-obesity effects in diet-induced obese mouse models, highlighting its therapeutic potential in both oncology and metabolic disease research. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
HDAC inhibitor
Marein is a natural compound with multifaceted pharmacological properties, including HDAC inhibition with an IC₅₀ of 100 μM. It exerts neuroprotective effects by preserving mitochondrial function and activating the AMPK signaling pathway. In HepG2 cells, Marein improves high glucose–induced insulin resistance by enhancing glucose uptake via the CaMKK/AMPK/GLUT1 pathway, promoting glycogen synthesis through the IRS/Akt/GSK-3β pathway, and suppressing gluconeogenesis via the Akt/FoxO1 axis. Additionally, Marein possesses antioxidative, antihypertensive, antihyperlipidemic, and antidiabetic properties, making it a promising candidate for metabolic and neurodegenerative disease research. -
HDAC inhibitor
Crebinostat is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor with IC₅₀ values of 0.7 nM (HDAC1), 1.0 nM (HDAC2), 2.0 nM (HDAC3), and 9.3 nM (HDAC6). It effectively induces acetylation of histone H3 and H4, and enhances the expression of Egr1, a cAMP response element-binding protein (CREB) target gene. In cultured neurons, Crebinostat increases the density of synapsin-1 puncta along dendrites, indicating enhanced synaptic connectivity. By modulating chromatin-mediated neuroplasticity, Crebinostat has been shown to improve memory performance in mice, supporting its potential for neuropsychiatric and cognitive disorder research. -
HDAC inhibitor
Bakkenolide A is a natural sesquiterpene lactone isolated from *Petasites tricholobus*. It exhibits anti-leukemic activity by modulating epigenetic and signaling pathways, specifically through inhibition of histone deacetylase 3 (HDAC3) and regulation of the PI3K/Akt signaling cascade. These combined effects contribute to its potential as a therapeutic agent in leukemia research.
