Catalog No.
Product Name
Application
Product Information
Citations
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HDAC inhibitor
MC1742 is a potent pan-HDAC inhibitor with broad activity across multiple HDAC isoforms, exhibiting IC₅₀ values of 0.1 μM (HDAC1), 0.11 μM (HDAC2), 0.02 μM (HDAC3), 0.007 μM (HDAC6), 0.61 μM (HDAC8), 0.04 μM (HDAC10), and 0.1 μM (HDAC11). It effectively increases acetylation of histone H3 and α-tubulin, markers of HDAC inhibition. MC1742 inhibits the growth of cancer stem cells (CSCs), and induces growth arrest, apoptosis, and differentiation, particularly in sarcoma CSC models, making it a promising candidate for targeting therapy-resistant cancer cell populations. -
HDAC6 inhibitor
SelSA is a selective and orally active histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 56.9 nM. It also inhibits ERK1/2 phosphorylation, contributing to its anticancer effects. SelSA suppresses the proliferation of breast cancer and hepatocellular carcinoma cells with IC₅₀ values ranging from 0.58 to 2.6 μM, inhibits migration and invasion of Huh7 cells, and induces apoptosis. In vivo, SelSA demonstrates significant antitumor activity, supporting its potential as a therapeutic agent for solid tumors. -
HDAC inhibitor
KH16 is a potent histone deacetylase (HDAC) inhibitor with low nanomolar activity, selectively targeting class I HDACs—HDAC1, HDAC2, and HDAC3—with IC₅₀ values ranging from 6 to 34 nM. It effectively induces apoptosis and exhibits broad-spectrum antitumor activity across cancer cells with diverse gene expression profiles, making it a promising candidate for epigenetic cancer therapy research. - 1,6,7-Trihydroxyxanthone is a potent anticancer compound that inhibits tumor cell proliferation and induces apoptosis. It downregulates the expression of Bmi-1, a known oncogenic regulator, while upregulating the protein levels of tumor suppressors p14 and p16. These effects highlight its potential as a therapeutic agent for targeting oncogenic pathways in cancer research.
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ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
HDAC6 inhibitor
AES-350 is a potent and orally bioavailable histone deacetylase 6 (HDAC6) inhibitor, with an IC₅₀ of 0.0244 μM and a Kᵢ of 0.035 μM. It also exhibits inhibitory activity against HDAC3 and HDAC8, with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 induces apoptosis in acute myeloid leukemia (AML) cells through HDAC inhibition, making it a promising compound for AML research and the development of epigenetic-based cancer therapies. -
POLA1-HDAC11 Inhibitor
GEM144 is a potent and orally bioavailable dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It promotes p53 acetylation, induces p21 activation, and triggers G1/S cell cycle arrest followed by apoptosis. GEM144 exhibits significant antitumor efficacy in human orthotopic malignant pleural mesothelioma xenograft models, highlighting its potential as a targeted therapeutic agent for aggressive thoracic malignancies. -
POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
TAK1 inhibitor
HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA). -
Casein Kinase inhibitor
BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies. -
SUV39H1 methyltransferase inhibitor
F5446 (Compound 1) is a selective small-molecule inhibitor of the histone methyltransferase SUV39H1. By reducing H3K9 trimethylation (H3K9me3) at the Fas promoter, F5446 upregulates Fas expression and enhances the sensitivity of colorectal carcinoma cells to Fas ligand (FasL)-induced apoptosis in vitro. In vivo, F5446 effectively suppresses the growth of human colorectal tumor xenografts, highlighting its potential as an epigenetic therapeutic agent in cancer treatment. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
PROTAC RIPK degrader
PROTAC RIPK Degrader-2 is a non-peptidic, VHL-based PROTAC that selectively targets the serine/threonine kinase RIPK2 for degradation. It promotes cancer cell death and ion channel activation, while also inhibiting key protein interactions involved in disease pathways, including those related to cancer and diabetes. -
HOX/PBX interaction antagonist
HXR9 is a cell-permeable peptide that functions as a competitive antagonist of the HOX/PBX interaction, disrupting the binding of HOX proteins (paralogues 1–8) to the transcription factor PBX. It selectively inhibits proliferation and induces apoptosis in cells with elevated HOXA/PBX3 expression, such as MLL-rearranged leukemic cells, making it a valuable tool for studying HOX/PBX-driven oncogenesis. -
GPX4 PROTAC Degrader
PROTAC GPX4 degrader-1 functions as a targeted protein degradation agent specifically for GPX4. It exhibits a DC50 of 0.03 μM in HT1080 cells, demonstrating potent activity in promoting the degradation of GPX4. This compound is applicable in research exploring the role of GPX4 in various cellular processes and the therapeutic potentials of targeting antioxidant defenses in disease models. -
PROTAC MDM2 Degrader
MD-222 is a first-in-class PROTAC degrader targeting MDM2. This compound contains ligands for both Cereblon and MDM2, facilitating the rapid degradation of MDM2 protein and subsequent activation of wild-type p53 in cellular contexts. Due to its mechanism of action, MD-222 exhibits notable anticancer properties, making it a valuable tool for research in cancer biology and therapeutic development. -
p53 Activator
C16-Ceramide is a natural small molecule that acts as a p53 activator by directly and selectively binding to the protein. This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate p53 activity facilitates investigations into cellular stress responses and the mechanisms underlying tumor suppression. -
Alkaloid
Conophylline is a vinca alkaloid derived from the leaves of the tropical plant Ervatamia microphylla. This compound functions as a differentiation inducer for pancreatic cells and demonstrates potent biological activity by suppressing hepatic stellate cells (HSC) while inducing apoptosis. It is of particular interest in research focused on pancreatic differentiation and the modulation of liver fibrosis. -
Rac1/Cdc42 Inhibitor
AZA1 is a potent dual inhibitor of Rac1 and Cdc42, key regulators of cell signaling pathways. This compound has been shown to induce apoptosis in prostate cancer cells while simultaneously inhibiting their proliferation, migration, and invasion. AZA1 serves as a valuable tool for research into the molecular mechanisms of prostate cancer progression and potential therapeutic interventions. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
PROTAC RIPK degrader
PROTAC RIPK degrader-6 is a Cereblon-based protein-targeting chimeric molecule designed for the degradation of RIP Kinase. This compound employs a RIP2 kinase inhibitor linked through a suitable spacer to a cereblon ligand, facilitating targeted proteolysis of RIPK. Prominent applications include investigations into kinase-related signaling pathways and the development of innovative therapeutic strategies for diseases associated with RIPK dysregulation. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
Apoptosis Inducer
epi-Eriocalyxin A is a diterpenoid compound that serves as an apoptosis inducer in colon cancer cells. It effectively inhibits the activation of ERK1/2 and JNK pathways, leading to the suppression of Bcl-2 expression. This compound is valuable for research focused on cancer treatment and the mechanisms of apoptosis. -
Cdc42 GTPase Inhibitor
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines. -
Monounsaturated Fatty Acid
Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
Anticancer Agent
(+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage. -
Ionophore
Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines . -
Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
Tubulin Inhibitor
Demecolcine is a potent tubulin inhibitor that effectively disrupts microtubule polymerization, exhibiting an IC50 value of 2.4 μM. By binding to tubulin dimers, Demecolcine exerts anti-mitotic effects, hindering cellular division. This compound is primarily utilized in research related to inflammatory disorders and various cancer pathways, making it valuable for studies focused on cell cycle regulation and targeted therapies. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
Cysteine Residues Modifier
N-Ethylmaleimide (NEM) is a potent chemical reagent that irreversibly alkylates free sulfhydryl groups, specifically targeting cysteine residues. This compound serves as an effective inhibitor of cysteine proteases and significantly affects phosphate transport in mitochondria. With an IC50 value of 6.3 μM, N-Ethylmaleimide is valuable for modifying cysteine residues in proteins and peptides, making it an essential tool in biochemical research and studies involving protein functionality and structure. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
Bcl-xL/Bcl-2 Inhibitor
BM-1244 is a selective inhibitor of Bcl-xL and Bcl-2, exhibiting Ki values of 134 nM and 450 nM, respectively. This compound induces apoptosis and suppresses tumor growth through the release of cytochrome C and Smac from mitochondria, leading to caspase-3 activation and PARP cleavage. BM-1244 has demonstrated synergistic effects with chemotherapy in vivo, making it a valuable research tool for studying colorectal cancer, acute myeloid leukemia, and gastric cancer. -
Bcl-2/Bcl-xl Inhibitor
Pelcitoclax is a potent inhibitor of Bcl-2 and Bcl-xl, designed to induce apoptosis in cancer cells. Its primary mechanism involves disrupting the anti-apoptotic activity of these proteins, leading to increased cell death in malignant tissues. Pelcitoclax is utilized in research to explore therapeutic strategies against various malignancies and to study apoptotic pathways in cellular models. -
Bcl-2/Bcl-xl Inhibitor
Lisaftoclax is a potent inhibitor of the anti-apoptotic proteins Bcl-2 and Bcl-xl. With IC50 values of 2 nM for Bcl-2 and 5.9 nM for Bcl-xl, Lisaftoclax demonstrates significant anti-tumor activity. This compound is primarily utilized in research focused on cancer therapy, particularly in studies exploring mechanisms of apoptosis and the role of Bcl-2 family proteins in tumor survival. -
RIPK3 Inhibitor
GSK-872 hydrochloride is a potent inhibitor of receptor-interacting protein kinase 3 (RIPK3), exhibiting an IC50 of 1.8 nM for binding to the RIP3 kinase domain and an IC50 of 1.3 nM for inhibiting its kinase activity. This compound effectively reduces RIPK3-mediated necroptosis and inhibits the cytoplasmic translocation and expression of HMGB1. Additionally, GSK-872 hydrochloride has been shown to alleviate brain edema and neurological deficits in models of early brain injury, making it a valuable tool for studying necroptosis and related pathophysiological processes. -
RIPK1 Inhibitor
TP-030-1 is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1). It demonstrates a high affinity for human RIPK1 with a Ki value of 3.9 nM and an IC50 of 4.2 μM for mouse RIPK1. This compound is valuable for investigating the mechanisms underlying inflammatory and neurodegenerative diseases, providing insights into potential therapeutic interventions. -
RIPK2 Inhibitor
CSLP37 is a selective inhibitor of receptor-interacting protein kinase 2 (RIPK2), exhibiting an IC50 of 16.3 nM. This compound effectively suppresses cellular responses mediated by NOD1 and NOD2, while showing no significant inhibitory activity against RIPK1 and RIPK3. CSLP37 is a valuable tool for research into inflammatory signaling pathways and the role of RIPK2 in various diseases. -
RIPK1 Inhibitor
Cl-Necrostatin-1 is a selective inhibitor of receptor-interacting protein kinase 1 (RIPK1). It effectively blocks TNF-α-induced necroptosis in Jurkat cells lacking FADD, with an EC50 of 180 nM, thereby preventing caspase activation linked to death-domain receptor signaling. Additionally, Cl-Necrostatin-1 has been shown to decrease infarct size in a mouse model of middle cerebral artery occlusion (MCAO), making it a valuable tool for research in cardiovascular and cerebrovascular pathologies. -
RIPK1 Inhibitor
ZB-R-55 is a potent orally active inhibitor of receptor-interacting protein kinase 1 (RIPK1). This compound exhibits significant potential in modulating cell death pathways and inflammation, making it a valuable tool for researching sepsis and other inflammatory conditions. Its ability to selectively inhibit RIPK1 supports investigations into therapeutic strategies for diseases characterized by dysregulated necroptosis. -
RIPK3 Inhibitor
RIPK3-IN-3 is a selective inhibitor of the receptor-interacting protein kinase 3 (RIPK3), with an IC50 of 10 nM. This compound effectively prevents the phosphorylation of Mixed Lineage Kinase (MLKL), thereby inhibiting oligomerization of p-MLKL and subsequently blocking necroptosis. Additionally, RIPK3-IN-3 has been shown to downregulate CXCL5 secretion and suppress migration and invasion in AsPC-1 cancer cells, making it a valuable tool for studying necroptosis and related pathways in cancer research. -
RIPK1 Inhibitor
TP-030-2 is a potent RIPK1 inhibitor, with a human Ki of 0.43 nM and a mouse IC50 of 100 nM. This compound is designed for research applications targeting necroptosis and inflammatory pathways, making it a valuable tool for investigating cell death mechanisms and disease processes related to RIPK1 signaling. Its high specificity and efficacy support investigations into therapeutic strategies for conditions involving dysregulated cell death. -
RIPK1 Inhibitor
SZM679 is a selective inhibitor of receptor-interacting protein kinase 1 (RIPK1) with a Kd value of 8.6 nM, demonstrating high specificity over RIPK3 (>5000 nM). This compound effectively reverses tumor necrosis factor-induced systemic inflammatory responses and reduces Tau hyperphosphorylation and neuroinflammation in the hippocampus and cortex. SZM679 has significant potential for research applications in Alzheimer's disease and other neurodegenerative disorders. -
RIPK1 Inhibitor
Necrostatin-34 is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1). It stabilizes the inactive conformation of RIPK1 by binding to a specific pocket within the kinase domain, thereby preventing its activation. This compound is primarily utilized in research to explore necroptosis and cell death pathways, making it valuable for studies in inflammation, neurodegeneration, and cancer. -
RIPK1 Inhibitor
RI-962 is a potent and selective inhibitor of receptor-interacting protein kinase 1 (RIPK1), exhibiting an IC50 value of 35.0 nM. This compound is applicable in research focused on neurodegenerative disorders and inflammatory diseases, where modulation of RIPK1 activity can provide insights into disease mechanisms and potential therapeutic strategies. -
RIPK2/ALK2 Inhibitor
OD36 hydrochloride is a potent inhibitor of receptor-interacting protein kinase 2 (RIPK2) and an effective modulator of activin receptor-like kinase 2 (ALK2), exhibiting an IC50 of 5.3 nM against RIPK2. This macrocyclic compound demonstrates strong binding affinity for the ALK2 kinase ATP pocket, with a Kd of 37 nM. OD36 hydrochloride is suitable for research applications focused on signaling pathways involving RIPK2 and ALK2, relevant in studying various diseases, including inflammation and cancer.
