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Catalog No.
Product Name
Application
Product Information
Citations
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PDE4 Inhibitor
GPD-1116 is a potent inhibitor of Phosphodiesterase (PDE) 4 and PDE1, demonstrating oral bioactivity. This compound effectively reduces smoke-induced apoptosis in lung cells, making it relevant for respiratory research. GPD-1116 shows promise in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary hypertension, supporting its potential therapeutic applications in pulmonary disorders. -
Hsp90-Cdc37 PPI Inhibitor
Hsp90-Cdc37-IN-4 is a selective inhibitor of the Hsp90-Cdc37 protein-protein interaction (PPI). This compound disrupts the interaction by inhibiting casein kinase 2 (CK2), leading to reduced phosphorylation of Cdc37 at Serine 13. In cellular assays, Hsp90-Cdc37-IN-4 has been shown to induce G0/G1 cell cycle arrest and activate apoptotic pathways via the mitochondria. Additionally, it exhibits significant anti-breast cancer properties, making it a valuable tool in cancer research. -
IDO/Tubulin Inhibitor
HI5 is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO) and tubulin, demonstrating an IC50 of 70 nM in HeLa cells. It effectively reduces kynurenine production, thereby promoting T cell activation and proliferation. Additionally, HI5 interferes with tubulin polymerization and migration, induces G2/M phase cell cycle arrest, and triggers apoptosis through a mitochondrial-dependent pathway, leading to increased reactive oxidative stress. HI5 is suitable for research in anticancer applications. -
HSP90 Inhibitor
HSP90-IN-13 is a potent inhibitor of Heat Shock Protein 90 (HSP90) with an IC50 of 25.07 nM. This compound exhibits multi-target activity, affecting key proteins such as Epidermal Growth Factor Receptor (EGFR), Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2), and Topoisomerase-2. HSP90-IN-13 promotes cell cycle arrest at the G2/M phase and induces apoptosis in MCF-7 cancer cells via a mitochondrial-mediated pathway, making it a valuable reagent for cancer research and therapeutic studies. -
MAO-B/Acetylcholinesterase Inhibitor
MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease. -
TrxR Inhibitor
TrxR-IN-6 is an inhibitor of thioredoxin reductase (TrxR), a key enzyme in maintaining the cellular redox balance. This compound induces the accumulation of reactive oxygen species (ROS), leading to mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and DNA damage. TrxR-IN-6 effectively promotes oxidative stress, resulting in apoptosis, making it a valuable tool for cancer research and studies focusing on oxidative stress mechanisms. -
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). -
PD-L1/NAMPT Inhibitor
PD-L1/Nampt-IN-1 is a dual inhibitor targeting PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50 values of 63 nM and 582 nM, respectively. This compound exhibits cross-species affinity with comparable KD values for human PD-L1 (52.6 nM) and mouse PD-L1 (49.1 nM). PD-L1/Nampt-IN-1 facilitates tumor growth inhibition by enhancing the tumor immune microenvironment, making it a valuable tool for research in melanoma studies. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-4 is a potent dual-target inhibitor of CYP51 and PD-L1, demonstrating IC50 values of 0.17 μM and 0.021 μM, respectively. This compound exhibits significant antifungal activity and is effective against drug-resistant fungal strains in vitro. CYP51/PD-L1-IN-4 is suitable for research applications focused on fungal infections and the interplay between fungal pathogens and immune checkpoint regulation. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
PDE4 Inhibitor
Morcamilast is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, exhibiting IC50 values of 1.28 nM for PDE4A1A, 2.33 nM for PDE4B1, and 1.63 nM for PDE4D2. This compound demonstrates significant anti-inflammatory activity by inhibiting the lipopolysaccharide (LPS)-induced release of pro-inflammatory cytokines, including TNF-α, IL-12/23p40, IL-23, and IL-17A in human peripheral blood mononuclear cells (PBMCs) and T cells. Morcamilast also exhibits antipruritic effects, making it a valuable tool for investigating psoriasis, atopic dermatitis, and various other inflammatory disorders. -
PDE1C Inhibitor
PDE1-IN-9 is a selective inhibitor of phosphodiesterase 1 (PDE1), demonstrating an IC50 of 11 nM for PDE1C. This compound significantly reduces the mRNA expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α, as well as iNOS, while inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 also showcases favorable metabolic stability in rat liver microsomes, making it a valuable tool for studying PDE1-related pathways and inflammatory responses. -
PDE4 Inhibitor
Mesopram is a selective phosphodiesterase (PDE) 4 inhibitor that effectively reduces the synthesis of pro-inflammatory cytokines, including TNF-α and IFN-γ. This compound has shown efficacy in alleviating Dextran sulfate sodium (DSS)-induced colitis in murine models, making it a valuable tool for research in chronic inflammatory diseases. Mesopram can be employed to investigate therapeutic strategies aimed at modulating inflammatory responses. -
MAO-A/DYRK1A Inhibitor
Norharmine is a Harmine analogue that functions as an inhibitor of monoamine oxidase A (MAO-A) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A). It exhibits weak inhibitory activity against MAO-A and demonstrates certain inhibitory effects on DYRK1A, positioning it as a valuable tool for research in neurobiology and cellular signaling pathways. Norharmine is useful in studies focusing on mood disorders and cognitive functions related to these kinase targets. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride is a potent inhibitor of phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. Additionally, it acts as an antagonist of the H1-histamine receptor, contributing to its anti-inflammatory properties. Fenspiride is primarily utilized in research related to respiratory diseases, offering insights into mechanisms of action and potential therapeutic applications. -
5-Lipoxygenase Inhibitor
Linetastine is a potent, orally active inhibitor of 5-Lipoxygenase, an enzyme critical in the synthesis of leukotrienes. By inhibiting this pathway, Linetastine demonstrates significant antihistamine activity, effectively reducing leukotriene B4 and C4 release from calcium ionophore-stimulated human leukocytes. This compound is particularly useful in research applications focused on inflammatory processes and allergic responses, providing insights into the modulation of leukotriene-mediated pathways. -
HSP Inhibitor
Apatorsen sodium is a 2'-methoxyethyl-modified antisense oligonucleotide targeting Hsp27. It effectively reduces Hsp27 mRNA and protein levels, disrupting stress-induced cytoprotective functions, promoting apoptosis, inhibiting tumor growth, and preventing metastasis. This compound is relevant for research applications in non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, and bladder cancer. -
Hsp90-Cdc37 PPI Inhibitor
DDO-5936 is a potent inhibitor of the Hsp90-Cdc37 protein-protein interaction. This compound specifically disrupts the chaperone-client complex, leading to altered protein folding and degradation pathways. Its biological activity makes DDO-5936 a valuable tool for research applications focused on colorectal cancer and other related therapeutic areas. -
HSPA5 Inhibitor
HM03 is a selective inhibitor of HSPA5 (Heat Shock Protein 70kDa, also known as Bip or Grp78). This compound exhibits significant anticancer activity, making it a valuable tool for cancer research. It can be utilized to study the role of HSPA5 in tumor progression and therapeutic resistance, providing insights into potential treatment strategies targeting this chaperone protein. -
Hsp90 Inhibitor
Zelavespib hydrochloride is a potent inhibitor of the heat shock protein 90 (Hsp90), exhibiting an IC50 of 51 nM in MDA-MB-468 cancer cell lines. This compound disrupts Hsp90 function, leading to the degradation of client oncoproteins, thereby demonstrating significant potential in cancer research. Zelavespib is utilized in studies focused on the therapeutic targeting of Hsp90 for various malignancies. -
Hsp70 Inhibitor
YM-1 is an orally active inhibitor of the heat shock protein 70 (Hsp70). This compound has been shown to induce apoptosis in HeLa cells while also up-regulating key regulatory proteins such as p53 and p21. Its effects on cell viability and protein expression make YM-1 a valuable tool for studying the role of Hsp70 in cancer biology and therapeutic applications. -
PfHsp90 Inhibitor
Ursolic acid acetate is a triterpenoid compound that inhibits Plasmodium falciparum heat shock protein 90 (PfHsp90) with a binding affinity (KD) of 8.16 μM. It exhibits cytotoxic effects on KB cells, with an IC50 value of 8.4 μM. This compound is suitable for applications in tumor research and antimalarial studies, providing a valuable tool for investigating the role of heat shock proteins in disease mechanisms. -
HSP70 Allosteric Inhibitor
MAL3-101 is a potent allosteric inhibitor of the heat shock protein 70 (HSP70), primarily acting by inhibiting the ATPase activity of HSP70 through disruption of the Hsp40 co-chaperone interaction. This compound has demonstrated significant biological activity in cellular models, making it a valuable tool for investigating the role of HSP70 in muscle invasive bladder cancer (MIBC) research. Researchers can utilize MAL3-101 to explore therapeutic strategies targeting this molecular chaperone in cancer treatment. -
HSP90 Inhibitor
Icapamespib hydrochloride is a selective inhibitor of HSP90, targeting epichaperome assembly with slow dissociation kinetics. This compound effectively disrupts disease-related protein interaction networks, reducing neurotoxic protein aggregation and hindering tumor cell survival signals. Icapamespib hydrochloride is valuable in research focused on neurodegenerative diseases, including Alzheimer's disease, along with various cancers, such as glioblastoma and metastatic breast cancer. -
HSP90 Inhibitor
Icapamespib is a selective inhibitor of HSP90 that effectively disrupts epichaperome formation through non-covalent binding, exhibiting slow dissociation kinetics. This compound is capable of crossing the blood-brain barrier, facilitating the disassembly of abnormal protein interaction networks and reducing neurotoxic protein aggregation. Icapamespib demonstrates potential in research applications focused on neurodegenerative diseases, including Alzheimer’s disease, as well as various cancers such as glioblastoma and metastatic breast cancer. -
Hsp90 Inhibitor
SNX-0723 is a potent Hsp90 inhibitor that exhibits anti-Plasmodium activity. It demonstrates notable binding affinity for human Hsp90 and Plasmodium falciparum Hsp90, with inhibition constants (Kis) of 4.4 nM and 47 nM, respectively. Additionally, SNX-0723 effectively inhibits liver-stage Plasmodium berghei ANKA parasites, with an EC50 value of 3.3 μM, making it a valuable tool for research into malaria treatment and Hsp90-related biological processes. -
HSP70 ATPase Inhibitor
Displurigen (NSC375009) is an HSP70 ATPase inhibitor that specifically targets HSPA8, disrupting the pluripotency of human embryonic stem cells. This compound effectively inhibits the ATPase activity of HSP70 with an IC50 of 225 μM, making it a valuable tool for research in stem cell biology and differentiation processes. Its mechanism of action provides insights into cellular signaling pathways related to stem cell maintenance and development. -
HSP90β Inhibitor
KUNB31 is a selective inhibitor of HSP90β, exhibiting a binding affinity with a Kd value of 0.18 μM. This compound disrupts the function of the HSP90β protein, which is implicated in the maturation and stabilization of client proteins involved in cancer and other diseases. KUNB31 is valuable for research focused on cellular stress responses, protein homeostasis, and therapeutic strategies targeting protein chaperones. -
Hsp90 Inhibitor
Hsp90-IN-37 is a potent inhibitor of heat shock protein 90 (Hsp90), demonstrating a 69% reduction in enzymatic activity. This compound exhibits significant antitumor properties, making it a valuable tool in cancer research. Hsp90-IN-37 can be utilized to explore the role of Hsp90 in cancer cell survival and proliferation, supporting efforts to develop targeted therapies. -
Hsp90 Inhibitor
3-Phenyltoxoflavin is an Hsp90 inhibitor that interacts with the Hsp90-TPR2A complex, exhibiting a dissociation constant (Kd) of 585 nM. This compound demonstrates significant anti-cancer properties, making it a valuable tool for cancer research. Its ability to inhibit Hsp90 function provides insights into the molecular mechanisms of cancer cell growth and survival, supporting studies aimed at developing targeted therapies. -
HSP90 Inhibitor
Hsp90-IN-17 hydrochloride is a potent inhibitor of Heat Shock Protein 90 (HSP90), a chaperone protein involved in protein folding and stabilization. This compound demonstrates significant biological activity by disrupting the chaperoning function of HSP90, leading to the degradation of oncogenic client proteins. Hsp90-IN-17 is primarily used in research applications focused on proliferative diseases, including various cancer types and neurodegenerative disorders, providing insights into therapeutic strategies targeting HSP90. -
HSP90 Inhibitor
HSP90-IN-23 is a potent inhibitor of heat shock protein 90 (HSP90) with an IC50 value of 9 nM. This compound effectively induces apoptosis in tumor cells and successfully arrests the cell cycle in the G0/G1 phase. HSP90-IN-23 is an invaluable tool for cancer research, facilitating the study of HSP90's role in tumorigenesis and potential therapeutic strategies. -
HSP70 Inhibitor
AP-4-139B is a potent inhibitor of HSP70, exhibiting an IC50 of 180 nM against human HSP70. Its mechanism involves direct binding to HSP70, leading to the inhibition of ATPase activity. By facilitating the phosphorylation of Beclin-1, AP-4-139B promotes autophagy. This compound has demonstrated significant antitumor activity in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma, making it a valuable tool for cancer research. -
Hsp90 Inhibitor
HSP90-IN-22 is an inhibitor of heat shock protein 90 (Hsp90) that exhibits significant antiproliferative activity in cancer cells. The compound demonstrates IC50 values of 3.65 μM in MCF7 breast cancer cells and 2.71 μM in SKBr3 breast cancer cells. This compound is valuable for research into cancer cell biology and the therapeutic potential of Hsp90 inhibition in cancer treatment. -
Fluorescently-tethered Hsp90 Inhibitor
HS-27 is a fluorescently-tethered inhibitor targeting Heat Shock Protein 90 (Hsp90), facilitating the assessment of surface Hsp90 expression on intact tissue specimens. Comprising core elements of SNX-5422 linked through a PEG spacer to a fluorescein derivative, HS-27 selectively binds to ectopically expressed Hsp90. This reagent is particularly valuable in breast cancer research, providing a tool for applications involving visualization and treatment strategies. -
Hsp27 Inhibitor
Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide that functions as a Heat Shock Protein 27 (Hsp27) inhibitor. By reducing Hsp27 mRNA and protein levels, Apatorsen disrupts stress-induced cytoprotective mechanisms, promotes apoptosis, inhibits tumor growth, and prevents metastasis. This compound is particularly relevant for research focused on non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, and bladder cancer. -
HSP90 Inhibitor
Aminohexylgeldanamycin (AHGDM) is a potent inhibitor of HSP90, a chaperone protein essential for the proper folding and function of many oncoproteins. This compound exhibits significant antiangiogenic and antitumor activities, making it a valuable tool in cancer research. Its ability to disrupt HSP90 function highlights its potential in the study of tumor biology and therapeutic interventions targeting heat shock proteins. -
HSP90 Inhibitor
CH5015765 is a potent HSP90 inhibitor that targets the N-terminal ATP binding site with a dissociation constant of 3.4 nM. This compound demonstrates significant antiproliferative activity, exhibiting IC50 values of 0.46 μM in HCT116 colorectal cancer cells and 0.57 μM in NCI-N87 gastric cancer cells. CH5015765 is suitable for research applications focused on cancer biology and therapeutic development. -
HSP90 Inhibitor
HSP90-IN-27 is a potent inhibitor of the heat shock protein 90 (HSP90), which plays a critical role in protein folding and stabilization of client proteins involved in cancer progression. This compound effectively disrupts HSP90 function, leading to the degradation of oncogenic proteins and subsequent inhibition of tumor growth. HSP90-IN-27 is applicable in cancer research, particularly in studies focused on targeted therapies and the molecular chaperone network. -
Hsp60-Hsp10 Inhibitor
[Au(TPP)]Cl is an inhibitor of the Hsp60-Hsp10 complex, which plays a critical role in protein folding and cellular stress responses. This compound demonstrates significant anticancer activity by disrupting the refolding process of misfolded proteins, thereby promoting cell apoptosis in cancerous cells. [Au(TPP)]Cl is valuable for research applications targeting cancer therapy and understanding the molecular mechanisms of chaperone functions. -
Hsp90 Inhibitor
Onalespib lactate is a highly potent inhibitor of heat shock protein 90 (Hsp90) with a Kd of 0.71 nM, demonstrating the capability to cross the blood-brain barrier. This compound effectively inhibits tumor cell proliferation, survival, and migration, while reducing the expression of key signaling proteins such as EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, and P-S6. With its significant antitumor activity, Onalespib lactate is particularly relevant for research into non-small cell lung cancer (NSCLC). -
HSP90 Inhibitor
HSP90-IN-11 is a potent inhibitor of HSP90, exhibiting strong inhibition of HSP90α activity. This compound demonstrates significant antiproliferative effects in colorectal cancer (CRC) and non-small cell lung cancer (NSCLC) cell lines, with IC50 values in the low double-digit nanomolar range. HSP90-IN-11 facilitates the rapid degradation of client proteins such as EGFR and Akt in NSCLC cells and induces a notable accumulation of sub-G1 phase cell populations, highlighting its potential for cancer research applications. -
Hsp90 inhibitor
BX-2819 is a potent inhibitor of Heat Shock Protein 90 (Hsp90) with an IC50 value of 41 nM. This compound effectively inhibits the proliferation of various cancer cell lines and has demonstrated significant antitumor activity in vivo, notably reducing the growth of NCI-N87 and HT-29 tumors in nude mouse models. BX-2819 is a valuable tool for research into cancer biology and potential therapeutic strategies targeting Hsp90. -
Hsp90a Inhibitor
CH5164840 is a potent inhibitor of the N-terminal domain of Hsp90a, exhibiting a high binding affinity with a Kd value of 0.52 nM. This compound demonstrates significant anti-proliferative effects against various human cancer cell lines, including HCT116 and NCI-N87, with IC50 values of 0.15 μM and 0.066 μM, respectively. Additionally, CH5164840 has an oral bioavailability profile with a half-life of 2.64 hours, indicating its potential for effective antitumor applications in therapeutic settings. -
Hsp90 Inhibitor
HSP90-IN-19 is a potent inhibitor of heat shock protein 90 (Hsp90), identified for its effective inhibitory activity with an IC50 value of 0.27 μM. This compound is relevant for studies investigating viral infections, neurodegenerative diseases, and inflammatory processes. Its ability to modulate cellular stress response pathways makes it a valuable tool in biochemical research and drug development efforts targeting Hsp90. -
Pan-PPAR Agonist, HIF-1α Inhibitor
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies. -
PPARγ Inhibitor
PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology. -
PPARγ inhibitor
SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism. -
PPARG Inhibitor
FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology.
