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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HCN2 Inhibitor
HCN2-IN-2 is a selective inhibitor of the HCN2 ion channel, characterized by an IC50 of 145 nM. This azaindazole derivative effectively blocks HCN2 channel activity, preventing abnormal firing in peripheral nociceptive neurons. HCN2-IN-2 is suited for research applications focused on pain modulation and the underlying mechanisms of nociceptive signaling. -
HCN2 Inhibitor
HCN2-IN-1 is a potent HCN2 inhibitor with an IC50 of 98 nM. This compound selectively targets hyperpolarization-activated cyclic nucleotide-gated channels, making it a valuable tool for investigating central nervous system (CNS) and psychiatric disorders. HCN2-IN-1 can facilitate research into the mechanisms underlying neuronal excitability and potential therapeutic strategies for related conditions. -
HCN2 Inhibitor
HCN2 modulator-6 is a potent inhibitor of the HCN2 ion channel, exhibiting an IC50 of 7 nM. This compound effectively suppresses HCN2 channel activity, making it a valuable tool for investigating mechanisms underlying pain, including inflammatory and neuropathic pain. Additionally, HCN2 modulator-6 is applicable in research focused on tinnitus, central nervous system disorders, psychiatric conditions, and mood disorders. -
HCN2 Inhibitor
HCN2-IN-5 is a potent HCN2 ion channel inhibitor with an IC50 of 9 nM, exhibiting minimal inhibitory activity on HCN4. This compound is valuable in the study of inflammatory diseases and neurological disorders, providing insights into the modulation of ion channel activity. Its specificity and potency make it a useful tool for elucidating the role of HCN2 in various physiological and pathological processes. -
AMPAR Inhibitor
TAT-GluA2 3Y is an AMPAR inhibitor that interferes with the endocytosis of AMPA receptors, thereby blocking long-term depression (LTD) at glutamatergic synapses. This peptide has been shown to mitigate pentobarbital-induced spatial memory deficits, highlighting its potential in studying synaptic plasticity and memory-related research applications. TAT-GluA2 3Y serves as a valuable tool for exploring the mechanisms underlying synaptic transmission and cognitive function. -
AQP2/CFTR Inhibitor
Steviol is a selective inhibitor of the aquaporin-2 (AQP2) and cystic fibrosis transmembrane conductance regulator (CFTR) proteins. This compound impedes renal cyst growth by inhibiting CFTR activity, which leads to decreased AQP2 expression and promotes the degradation of both AQP2 and CFTR. Steviol is relevant for research focused on polycystic kidney disease and mechanisms underlying renal cyst development. -
EHD4 ATPase Inhibitor
ATPase-IN-4 is a selective inhibitor of EHD4 ATPase activity, with an IC50 value of 0.92 μM. This compound also exhibits inhibitory effects on the ATPase activity of EHD2. ATPase-IN-4 is valuable for research applications focused on understanding the role of EHD proteins in cellular processes and membrane trafficking. -
ATPase Inhibitor
ATPase-IN-2 is a potent ATPase inhibitor with an IC50 value of 0.9 μM. It effectively inhibits the glycohydrolase activity of Clostridium difficile toxin B (TcdB) with an AC50 value of 30.91 μM. This compound serves as a valuable tool for studying ATP-related mechanisms and elucidating the role of ATPases in various biological processes. -
CF1 ATPase Inhibitor
Ovothiol A disulfide is a specific inhibitor of CF1 ATPase, targeting its light-activated function. This compound has been shown to effectively inhibit ATP synthesis in photophosphorylation processes, making it a valuable tool for studying energy transduction in photosynthetic organisms. Its role in modulating ATPase activity provides insights into the regulation of bioenergetics and enzyme kinetics in various biological systems. -
Mitochondrial F0F1-ATPase Inhibitor
Isoapoptolidin is an inhibitor of the mitochondrial F0F1-ATPase, exhibiting a Ki greater than 100 μM and selective action towards mitochondrial complex V. This compound is valuable for investigating mitochondrial energy metabolism-related disorders, including cancer and neurodegenerative diseases. Its inhibitory properties facilitate studies on the role of ATP synthase in cellular energy regulation. -
Dual MDR1/BCRP Inhibitor
CP-100356 hydrochloride is a potent dual inhibitor of MDR1 (P-glycoprotein) and BCRP, featuring IC50 values of 0.5 µM and 1.5 µM for the inhibition of MDR1-mediated transport of Calcein-AM and BCRP-mediated transport of Prazosin, respectively. It also exhibits off-target activity as a weak inhibitor of OATP1B1 with an IC50 of approximately 66 µM, while showing no significant inhibition against MRP2 or major human P450 enzymes (IC50 > 15 µM). This compound is useful in studying drug transport dynamics and enhancing the bioavailability of therapeutic agents in pharmacological research. -
BCRP Inhibitor
Ac32Az19 is a selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating a potent inhibitory effect with an EC50 value of 13 nM in BCRP-overexpressing HEK293/R2 cells. This high affinity and nontoxic profile make Ac32Az19 a valuable tool for research applications focused on drug transport mechanisms and multidrug resistance in cancer studies. Its specificity for BCRP allows for detailed investigations into therapeutic strategies and the modulation of drug pharmacokinetics. -
ABCG2/BCRP Inhibitor
Efflux inhibitor-1 is a pyrazolo[1,5-a]pyrimidine compound that selectively inhibits the ABCG2/BCRP transporter. With IC50 values of 0.45 μM for ABCG2/BCRP and 2.17 μM for ABCB1, this inhibitor is a valuable tool for studying drug efflux mechanisms and multidrug resistance. It is useful in research applications focused on cancer pharmacology and the modulation of drug absorption and resistance pathways. -
BCRP Inhibitor
ML753286 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an IC50 of 0.6 μM. This compound demonstrates high permeability and moderate clearance in liver S9 fractions from both rodent and human sources. Additionally, ML753286 remains stable across species in plasma, making it a valuable tool for studies investigating drug resistance mechanisms and pharmacokinetics in cancer research. -
BCRP Inhibitor
Ac22(Az8)2 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an EC50 value of 1-2 nM. This compound effectively restores drug sensitivity in BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, thereby blocking drug efflux and enhancing intracellular drug accumulation. Ac22(Az8)2 is a valuable tool for investigating BCRP-mediated mechanisms in multidrug-resistant cancers. -
BCRP Inhibitor
Pentamethoxymorin is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2), demonstrating significant potency with IC50 values of 5.98 μM and 5.94 μM in the Hoechst 33342 and Pheophorbide A assays, respectively. This compound showcases a preference for BCRP over other efflux transporters such as P-glycoprotein and MRP1. Pentamethoxymorin is valuable for research focusing on cancer resistance mechanisms and potential therapeutic interventions in breast cancer. -
MDR1/BCRP Inhibitor
CP-100356 is a dual inhibitor of MDR1 (P-glycoprotein) and BCRP, exhibiting IC50 values of 0.5 µM and 1.5 µM, respectively, for the inhibition of MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport. Additionally, CP-100356 shows weak inhibition of the OATP1B1 transporter, with an IC50 of approximately 66 µM, while demonstrating minimal inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM). This compound is valuable for research applications targeting drug resistance mechanisms and transport protein interactions in pharmacology and toxicology studies. -
BCRP/ABCG2 Inhibitor
Butein tetramethyl ether is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2) that demonstrates potent biological activity. It has been shown to inhibit BCRP in MCF-7 MX and MDCK cell lines, with IC50 values of 2.2 μM and 1.03 μM, respectively. This compound is a valuable tool for research investigating the mechanisms of cancer resistance and could provide insights into therapeutic strategies for overcoming drug resistance in cancer treatments. -
ABCG2 (BCRP) Inhibitor
UR-MB108 is a selective inhibitor of ABCG2 (BCRP) with an IC50 value of 79 nM. This compound demonstrates high potency in inhibiting the efflux activity of the ABCG2 transporter. UR-MB108's stability in blood plasma enhances its potential for various biological applications, including studies on drug absorption and resistance in cancer research. -
P-gp/BCRP Inhibitor
P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models.
