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Catalog No.
Product Name
Application
Product Information
Citations
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human ENT4 inhibitor
hENT4-IN-1 is a selective inhibitor of the human equilibrative nucleoside transporter 4 (ENT4), exhibiting an IC50 of 74.4 nM. This compound is crucial for investigating the biological roles of ENT4 in cellular nucleoside transport and metabolism. Its application extends to studies evaluating the impact of ENT4 inhibition on various physiological and pathological processes, making it a valuable tool for research in cancer biology and therapeutic development. -
ENT2 Inhibitor
FPMINT is a potent, irreversible, and non-competitive inhibitor of Equilibrative Nucleoside Transporters (ENTs), with a higher selectivity for ENT2 compared to ENT1. By effectively blocking ENT2, FPMINT significantly impacts uridine uptake, making it a valuable tool in studies related to nucleoside transport mechanisms. Its application in research can aid in elucidating the physiological roles of ENT2 in various biological processes. -
Adenosine reuptake inhibitor
Dilazep is an adenosine uptake inhibitor that enhances the effects of adenosine, leading to cerebral and coronary vasodilation. This compound not only reduces ischemic damage but also inhibits platelet aggregation and the membrane transport of nucleosides. Dilazep is useful in research applications focused on cardiovascular physiology and neuroprotection. -
hCNT1 Inhibitor
dMeThPmR is a selective inhibitor of the human nucleoside transporter 1 (hCNT1), exhibiting a potent inhibitory constant (Ki) in the range of 0.3-0.98 μM. While dMeThPmR shows minimal inhibition of hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM), it effectively protects cells from the cytotoxic effects of nucleoside drugs. This compound is valuable for research on cancer and related therapies, providing insights into nucleoside transport mechanisms and drug interactions. -
hCNT1 Inhibitor
MeThPmR is a potent and selective inhibitor of the human nucleoside transporter 1 (hCNT1) with a Ki ranging from 0.16 to 0.69 μM. It exhibits minimal inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR has been demonstrated to provide protection against the cytotoxic effects of nucleoside drugs, making it a valuable tool for cancer research applications. -
P-glycoprotein Inhibitor
NSC 23925B is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in multidrug resistance in cancer cells. This compound effectively reverses P-glycoprotein-mediated resistance and shows moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B is valuable for research focused on overcoming multidrug resistance in cancer therapy and studying P-glycoprotein's role in drug disposition. -
P-glycoprotein Inhibitor
Dofequidar fumarate is a potent P-glycoprotein (P-gp) inhibitor that also targets multidrug resistance-associated protein-1 (MDR-1). This quinoline compound effectively reverses multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. By blocking the efflux of chemotherapeutic agents, Dofequidar fumarate increases drug concentration within cancer cells, thereby enhancing the efficacy of chemotherapy. Its application is particularly relevant in cancer research focused on overcoming drug resistance. -
P-glycoprotein Inhibitor
Reversin 121 is a potent P-glycoprotein inhibitor that enhances the ATPase activity of the MDR1 gene product. By reversing P-glycoprotein-mediated multidrug resistance, it plays a critical role in overcoming drug resistance in cancer therapies. This compound is valuable for research applications focused on enhancing the efficacy of anticancer drugs in resistant cancer cell lines. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
P-Glycoprotein Inhibitor
Boeravinone B is a dual inhibitor of the NorA efflux pump in Staphylococcus aureus and human P-glycoprotein. This compound exhibits significant anti-biofilm activity and reduces intracellular bacterial invasion. Additionally, Boeravinone B demonstrates potential anti-aging and anti-apoptotic effects under oxidative stress conditions, making it a valuable reagent for research in microbiology and cellular aging pathways. -
P-glycoprotein Inhibitor
PGP-4008 is a selective inhibitor of P-glycoprotein (Pgp), known for its role in multidrug resistance (MDR) in cancer cells. This compound demonstrates significant antitumor activity by enhancing the efficacy of chemotherapeutic agents, particularly Doxorubicin, in murine models characterized by Pgp-mediated resistance. PGP-4008 is valuable for research into overcoming drug resistance in cancer therapy and the modulation of pharmacokinetics in oncology. -
P-glycoprotein Inhibitor
WS-898 is a potent P-glycoprotein inhibitor that effectively reverses paclitaxel resistance in various drug-resistant cancer cell lines, including SW620/Ad300, KB-C2, and HEK293/ABCB1, with IC50 values of 5.0, 3.67, and 3.68 nM, respectively. This compound serves as a valuable tool for research focused on overcoming multidrug resistance in cancer therapeutics. Its ability to inhibit ABCB1 transport activity makes it an important reagent for studies aimed at enhancing the efficacy of chemotherapeutic agents. -
P-gp Inhibitor
YS-370 is a potent and selective inhibitor of P-glycoprotein (P-gp) that exhibits oral bioavailability. It facilitates the P-gp ATPase activity while demonstrating moderate inhibition of CYP3A4. This compound effectively reverses multidrug resistance (MDR) in cell lines such as SW620/AD300 and HEK293T-ABCB1, particularly in conjunction with paclitaxel, leading to enhanced antitumor efficacy. YS-370 is valuable for research focused on overcoming drug resistance in cancer therapy. -
P-gp Inhibitor
Tariquidar dihydrochloride is a potent and selective inhibitor of P-glycoprotein (P-gp), exhibiting a high affinity with a Kd of 5.1 nM. This compound significantly enhances the bioavailability of co-administered drugs by inhibiting P-gp-mediated drug efflux. It is widely used in research to investigate the roles of P-gp in pharmacokinetics, drug-drug interactions, and multidrug resistance in cancer therapies. -
P-gp Inhibitor
OY-101 is a potent and orally active inhibitor of P-glycoprotein (P-gp). This compound demonstrates the ability to sensitize drug-resistant tumors, effectively reversing multidrug resistance in cancer cells. With improvements in water solubility, cytotoxicity, and reversal activity compared to Tetrandrine, OY-101 represents a valuable tool in cancer research and development of therapeutic strategies for overcoming drug resistance. -
ABCB1 Inhibitor
Tariquidar dimesylate is a potent ABCB1 inhibitor targeting P-glycoprotein (P-gp). By binding to P-glycoprotein, it effectively increases the concentration of therapeutic agents within the brain, inhibiting their active transport out of cerebral tissue. This compound is invaluable for investigating blood-brain barrier permeability and understanding mechanisms of multidrug resistance in cancer and neurological research. -
P-glycoprotein Inhibitor
Encequidar mesylate hydrochloride is a selective inhibitor of P-glycoprotein (MDR1), which plays a crucial role in drug resistance. This compound enhances the anti-tumor efficacy of Paclitaxel in various mouse tumor models, making it valuable for cancer research. Encequidar mesylate hydrochloride is primarily utilized to study drug interactions and to evaluate therapeutic strategies aimed at overcoming multidrug resistance in cancer treatment. -
P-gp Inhibitor
P-gp Inhibitor 17 is a selective inhibitor of P-glycoprotein (P-gp), directly targeting its transmembrane domain to modulate its activity. This compound is particularly useful for investigating P-gp-mediated multidrug resistance in cancer cells, providing insights into therapeutic strategies for overcoming resistance in oncology research. Its role in enhancing drug bioavailability and efficacy makes it a valuable tool for studying tumor cell behavior and treatment response. -
P-gp Inhibitor
P-gp Inhibitor 13 specifically targets P-glycoprotein (P-gp), functioning as an inhibitor to reverse P-glycoprotein-mediated drug resistance. This compound has demonstrated effectiveness in overcoming paclitaxel resistance in A2780/T cells, making it a valuable tool in cancer research. Its applications extend to the study of advanced acute myeloid leukemia, providing insights into therapeutic strategies for overcoming resistance in this malignancy. -
P-gp Inhibitor
P-gp inhibitor 14 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing P-gp-mediated multidrug resistance with an EC50 value of 48.74 nM. This compound demonstrates a weak inhibitory effect on CYP3A4 activity, making it a useful agent for enhancing the efficacy of chemotherapeutics in resistant cancer cells. Its primary applications include studies on drug transport mechanisms and overcoming resistance in multidrug-resistant tumors. -
P-gp Inhibitor
Clausarin is a selective P-glycoprotein (P-gp) inhibitor that effectively obstructs the P-gp-mediated efflux of chemotherapeutic agents. It demonstrates significant inhibition of daunorubicin efflux in K562/R7 human leukemia cells that overexpress P-gp, with Cyclosporin A serving as a positive control. Isolated from the roots of Citrus sinensis (sweet orange), Clausarin is a valuable reagent for research focused on overcoming multidrug resistance (MDR) in cancer therapies. -
Calcium Channel Inhibitor
McN5691 is a voltage-sensitive calcium channel inhibitor that selectively blocks calcium influx through L-type calcium channels. This action leads to reduced calcium-dependent cellular events, making it a valuable tool for investigating calcium signaling pathways. McN5691 is particularly useful in research focused on cardiovascular physiology and the modulation of muscle contraction mechanisms. -
Calmodulin inhibitor
Kobusin is a bisepoxylignan that functions as a calmodulin inhibitor. It is known to activate cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CaCC) while inhibiting the ANO1/ CaCC channel. This compound is valuable for research applications aimed at understanding calcium signaling and chloride transport mechanisms in various biological systems. -
CAL/CFTR Inhibitor
PGD97 is a selective cyclic peptide inhibitor that targets the CAL/CFTR interactions, exhibiting a KD value of 6 nM for its desulfide cyclized form at the CAL PDZ domain. Demonstrating a selectivity of ≥ 130-fold compared to NHERF1/2 PDZ domains, PGD97 effectively stabilizes F508del-CFTR at the cell membrane, enhancing CFTR function essential for maintaining fluid homeostasis in the lung. This compound is valuable for research applications focused on cystic fibrosis. -
Chloride Channel Inhibitor
R(+)-Methylindazone is a potent inhibitor of epithelial chloride channels. This compound effectively disrupts the interaction between Nef and the single-domain antibody Nef-sdAb19, demonstrating its ability to influence chloride channel activity. R(+)-Methylindazone is valuable for research exploring chloride channel regulation and the role of Nef in various biological processes. -
Chloride Channel Inhibitor
Ani9 is a selective inhibitor of the ANO1 chloride channel, exhibiting an IC50 of 77 nM. This compound effectively modulates smooth muscle contractions in murine models, making it a valuable tool for research on pathophysiological conditions such as tumors. Its inhibitory effects on chloride channels propose potential applications in studies targeting gastrointestinal disorders and related diseases. -
ANO1 Inhibitor
DFBTA is a potent inhibitor of ANO1 (anoctamin-1), a calcium-activated chloride channel, with an IC50 of 24 nM. This compound exhibits analgesic properties and demonstrates efficacy in models of inflammatory pain. It is a valuable reagent for research in pain pathways and the pharmacological modulation of ion channels. -
ClC-1 Inhibitor
NMD670 is an orally active inhibitor of the skeletal muscle chloride channel ClC-1, exhibiting an EC50 of 1.6 μM. This compound enhances neuromuscular transmission and contributes to improvements in muscle contraction and strength. NMD670 is valuable for research applications focused on muscle weakness and fatigue. -
Chloride Channel Inhibitor
MONNA is a potent inhibitor of the transmembrane protein 16A (TMEM16A, Anoctamin-1) with an IC50 of 80 nM. It effectively induces vasorelaxation in rodent resistance arteries, demonstrating its ability to modulate vascular tone regardless of chloride ion presence. This compound is valuable for research focused on chloride channel functions and their roles in cardiovascular physiology. -
ANO1 Inhibitor
ANO1-IN-4 is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), exhibiting an IC50 of 0.030 µM. This compound demonstrates favorable metabolic stability in rat liver microsomes, making it suitable for in vivo applications. ANO1-IN-4 effectively inhibits spontaneous contractions in mouse isolated ileum, indicating its potential for studies related to gastrointestinal motility and related disorders. -
TMEM16A Inhibitor
T16A(inh)-C01 is a potent inhibitor of the TMEM16A (ANO1) chloride channel. It effectively blocks chloride ion transport mediated by ANO1 with an IC50 of 8.4 μM, while maintaining normal calcium signaling pathways. This compound is valuable for studying the physiological roles of TMEM16A in various cellular processes and examining its potential relevance in disease models. -
ClC-ec1 Inhibitor
OADS is a selective inhibitor of the chloride channel antiporter ClC-ec1, exhibiting an IC50 value of 29 μM. This compound specifically interferes with the ClC-ec1 antiporter pathway, while showing no inhibitory effects on the ClC-1 channel. OADS is utilized in research related to osteoporosis, as well as various neurodegenerative and cardiovascular diseases, facilitating the study of these critical health conditions. -
Chloride Channel Inhibitor
NS3736 is an orally bioavailable inhibitor of chloride channels, specifically targeting the CIC-7 channel in osteocytes. This compound effectively blocks osteoclast acidification and resorption in vitro, exhibiting an IC50 of 30 μM. In preclinical studies using a rat model of ovariectomy-induced osteoporosis, NS3736 has demonstrated the ability to enhance bone strength and increase bone density, making it a valuable tool for researching osteoporosis. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
Chloride Channel Inhibitor
NS5818 is a potent chloride channel inhibitor that effectively disrupts acidification and bone resorption processes. Its mechanism of action makes it a valuable tool for studying osteoporosis and associated bone metabolic disorders. Researchers can utilize NS5818 to gain insights into chloride channel functions and their implications in bone health. -
Chloride Channel Inhibitor
Alilusem potassium is a selective chloride channel inhibitor known for its diuretic properties. Studies have demonstrated its effectiveness in reducing free water clearance while enhancing sodium and chloride excretion in urine during water diuresis in anesthetized canine models. Additionally, Alilusem potassium, when administered with Furosemide or Hydrochlorothiazide, further diminished free water clearance. This compound has also been shown to inhibit lumen-positive transepithelial voltage and chloride flux across isolated rabbit cortical thick ascending limbs of Henle, making it a valuable tool for research in renal physiology and electrolyte transport mechanisms. -
EAAT Inhibitor
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters (EAATs), specifically targeting EAAT1, EAAT2, and EAAT3 with IC50 values of 70 μM, 6 μM, and 6 μM, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, demonstrating Ki values of 42 μM and 5.7 μM, respectively. Additionally, DL-TBOA competitively blocks EAAT4 and EAAT5 with Ki values of 4.4 μM and 3.2 μM, respectively. This reagent is valuable for studying excitatory neurotransmission and related pathologies in research applications. -
Human EAAT2 Inhibitor
WAY-213613 hydrochloride is a potent and selective inhibitor of the human excitatory amino acid transporter 2 (EAAT2). With an IC50 value of 85 nM, it effectively modulates glutamate transport, making it a valuable tool for investigating glutamatergic signaling in the central nervous system. This compound is suitable for research applications exploring neurobiology and potential therapeutic interventions related to neurodegenerative diseases. -
EAAT1 Inhibitor
UCPH-102 is a highly selective inhibitor of the excitatory amino acid transporter 1 (EAAT1), exhibiting an IC50 value of 0.43 µM. This compound demonstrates significant anti-proliferative effects on T-cell acute lymphoblastic leukemia (T-ALL) cells. Furthermore, UCPH-102's favorable blood-brain barrier permeability makes it a valuable tool for research in neurodegenerative diseases such as amyotrophic lateral sclerosis and Alzheimer’s disease, as well as conditions related to chronic pain and obsessive-compulsive disorder. -
EAAT Inhibitor
L-threo-3-Hydroxyaspartic acid functions as a selective inhibitor of excitatory amino acid transporters (EAATs), exhibiting inhibitory constants (Kis) of 11, 19, and 14 μM for EAAT1, EAAT2, and EAAT3, respectively, in HEK293 cell lines. This compound plays a crucial role in the study of neurotransmitter regulation and excitotoxicity, making it valuable for research related to neurological disorders and synaptic transmission. Its ability to modulate glutamate signaling contributes to understanding potential therapeutic pathways for conditions such as epilepsy and neurodegenerative diseases. -
EAAT3 Inhibitor
SLC1A1/EAAT3-IN-1 is a selective inhibitor of the excitatory amino acid transporter 3 (EAAT3), exhibiting an IC50 of 7.2 μM for human EAAT3 while showing significantly reduced inhibition of EAAT1, 2, and 4 (IC50: ~250 μM). This compound is primarily utilized in research related to psychiatric disorders, including obsessive-compulsive disorder and schizophrenia, and can aid in the investigation of neurotransmitter dynamics and therapeutic strategies targeting EAAT3. -
EAAT Inhibitor
DL-TBOA ammonium is a selective inhibitor of excitatory amino acid transporters (EAATs), demonstrating IC50 values of 70 μM, 6 μM, and 6 μM for EAAT1, EAAT2, and EAAT3, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 42 μM and 5.7 μM. Additionally, DL-TBOA ammonium competitively inhibits EAAT4 and EAAT5, featuring Ki values of 4.4 μM and 3.2 μM, respectively. Its distinct mechanism renders it a valuable tool for studies on excitatory neurotransmission and the role of glutamate transporters in neurological research. -
EAAT2/4 Inhibitor
(±)-threo-3-Methylglutamic acid is a potent inhibitor of excitatory amino acid transporters EAAT2 and EAAT4. It functions as an ionotropic glutamate receptor agonist and is effective in inhibiting glutamate uptake in rod outer segments. This compound is valuable for research applications focusing on glutamatergic signaling and transport mechanisms in the nervous system. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes. -
HCN1 Inhibitor
RO-275 is a potent and selective HCN1 inhibitor, demonstrating IC50 values of 0.046 µM for HCN1, while showing significantly lower activity against HCN2 (14.3 µM), HCN3 (4.6 µM), and HCN4 (13.9 µM). This compound has been shown to effectively rescue impaired working memory, highlighting its potential utility in researching cognitive dysfunction associated with various brain disorders. RO-275 serves as a valuable tool for investigations into HCN1-related pathways and their implications in neurobiology. -
HCN2 Inhibitor
HCN2-IN-3 is an orally active inhibitor of HCN2 ion channels. It effectively reduces the activity of HCN2, making it valuable for research into pain mechanisms, tinnitus, and various central nervous system disorders. Additionally, HCN2-IN-3 has potential applications in studies focusing on mental illnesses and mood-related conditions. -
HCN2 Inhibitor
HCN2-IN-6 is a selective inhibitor of the HCN2 ion channel, demonstrating an IC50 value of 7 nM. It exhibits minimal inhibition of HCN4, making it a valuable tool for studying HCN2-specific pathways. This reagent is suitable for research into inflammatory diseases and neurological disorders, facilitating the exploration of potential therapeutic strategies targeting these conditions. -
HCN Inhibitor
pan-HCN-IN-1 is a potent inhibitor of the hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, exhibiting an IC50 value of 58 nM. This compound effectively attenuates the voltage sag response and enhances excitatory postsynaptic potential (EPSP) summation in ex vivo rat brain slices. It serves as a valuable tool for investigating the role of HCN1 channels in neuronal excitability and synaptic integration in various research applications. -
HCN Channel Inhibitor
MS7710 is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. It effectively reduces HCN channel-mediated Ih current, leading to decreased firing frequency and burst activity in dopaminergic neurons within the ventral tegmental area. Research has demonstrated that MS7710 ameliorates deficits in social interaction and cognitive flexibility related to reward processing in mice subjected to chronic social defeat stress. This compound is valuable for studies focusing on major depressive disorder and its underlying mechanisms. -
HCN2 Inhibitor
HCN2-IN-4 is an orally active inhibitor of the HCN2 ion channel, which plays a crucial role in neuronal excitability and rhythmic activity. This compound effectively inhibits HCN2 channel activity, making it a valuable tool for investigating its involvement in pain mechanisms, tinnitus, and various central nervous system disorders. Researchers may utilize HCN2-IN-4 to explore therapeutic strategies targeting these conditions.
