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Catalog No.
Product Name
Application
Product Information
Citations
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P-glycoprotein Inhibitor
Niguldipine monohydrochloride is a selective P-glycoprotein inhibitor known for its action as a calcium channel blocker. It demonstrates significant anticancer properties by inhibiting Cav 3.2, with an IC50 of 0.9 μM. This compound is primarily utilized in tumor research to explore its effects on drug resistance and the transport of therapeutic agents across cellular membranes. -
Nav1.2 Inhibitor
Nav1.2-IN-2 is a potent inhibitor of the voltage-gated sodium channel Nav1.2, demonstrating an IC₅₀ of 0.18 μM for channel inactivation. It effectively reduces both the amplitude and frequency of spontaneous synchronous calcium oscillations with IC₅₀ values of 0.38 μM and 0.88 μM, respectively. Additionally, Nav1.2-IN-2 inhibits calcium influx triggered by Veratridine with an IC₅₀ of 1.89 μM. This reagent is relevant for research into neurological disorders such as epilepsy. -
Calcium Channel Inhibitor
Piprofurol is a potent calcium channel inhibitor that effectively reduces calcium-induced contractions in isolated potassium depolarized rat aorta preparations in a concentration-dependent manner. This compound demonstrates the ability to relax K+-induced contractions in both dog coronary arteries and rabbit basilar arteries. Additionally, Piprofurol exhibits a negative inotropic effect on guinea-pig papillary muscle, with an EC50 value of 5 μM, highlighting its potential utility in cardiovascular research and related studies. -
Calcium Channel Inhibitor
(-)-Praeruptorin A is a natural product derived from the roots of Peucedanum praeruptorum Dunn, functioning as a calcium channel inhibitor. This compound induces relaxation of ileum and tracheal smooth muscles by activating the NO/cGMP signaling pathway. Its significant therapeutic potential in hypertension is primarily attributed to its capacity to block Ca2+-influx, making it a valuable reagent for research in cardiovascular pharmacology. -
Calcium Channel Inhibitor
Ro 18-3981 is a dihydropyridine compound that selectively inhibits calcium channels in cardiac tissues. It demonstrates enhanced inhibitory potency at depolarized membrane potentials, with an IC50 value of 2.3 nM at -20 mV and 100 nM at -50 mV. This compound is useful for studying the role of calcium signaling in cardiac physiology and related pathologies. -
Calcium Channel Inhibitor
R 56865 is a calcium channel inhibitor that offers cardiomyocyte protection against digitoxin (ouabain)-induced myocardial calcium overload. This compound demonstrates a significant protective effect against digitoxin-induced intoxication, as evidenced in studies utilizing guinea pig papillary muscle. R 56865 is primarily utilized in research related to cardiac function and the mechanisms of arrhythmias. -
UT-B Inhibitor
UT-B-IN-1 is a reversible, competitive inhibitor targeting the urea transporter-B (UT-B) with IC50 values of 10 nM for human and 25 nM for mouse UT-B. It demonstrates low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 significantly increases urine output and reduces urine osmolality in murine models, making it a valuable tool for research into diuretic mechanisms and kidney function studies. -
UT-A Inhibitor
PU-48 is a selective inhibitor of urea transporters A (UT-A), exhibiting an IC50 of 0.32 μM. This compound demonstrates significant diuretic activity in mouse models while showing minimal cytotoxicity. PU-48 presents a valuable tool for investigating renal physiology and has potential applications in the development of diuretic therapies. -
UT-A1/UT-B Urea Transporter Inhibitor
UTA1inh-D1 is a selective inhibitor of the UT-A1 and UT-B urea transporters, exhibiting IC50 values of 3.8 μM and 15 μM, respectively. This compound shows potential in the study of refractory edema conditions, including congestive heart failure and cirrhosis. Its unique mechanism of action makes it a valuable tool for exploring urea transport modulation in various pathological contexts. -
UT-A1/UT-B Inhibitor
UTA1inh-A1 is a selective inhibitor of urea transporters UT-A1 and UT-B, demonstrating IC50 values of 3.3 μM and 16 μM, respectively. This compound is primarily utilized in research focused on urea transport and its implications in diuretic therapy. UTA1inh-A1 aids in elucidating the physiological roles of urea transporters and their potential as therapeutic targets for urea-related conditions. -
UT-A Inhibitor
UTA1inh-C1 is a selective inhibitor of the urea transporter UT-A, demonstrating an IC50 of 4.2 μM. This compound effectively modulates urea transport, making it a valuable tool for studying renal physiology and urea homeostasis. Its application in research can help elucidate the role of UT-A in various physiological processes and the impact of urea transport dysregulation in pathological conditions. -
VDAC1 Inhibitor
VBIT-4 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity of 17 μM. This compound is recognized for its potential to inhibit apoptosis, making it suitable for therapeutic investigations in apoptosis-related conditions, including neurodegenerative and cardiovascular diseases. Researchers may utilize VBIT-4 to explore its effects on cell survival and disease progression in relevant biological models. -
VDAC1 Inhibitor
VBIT-12 is a potent inhibitor of Voltage-Dependent Anion Channel 1 (VDAC1) that functions by directly binding to the channel and preventing its oligomerization. This interaction effectively inhibits the pro-apoptotic actions mediated by VDAC1. VBIT-12 is valuable in studies aimed at elucidating the role of VDAC1 in apoptosis and mitochondrial function, making it a key reagent for research in cell death pathways and mitochondrial-related diseases. -
HK2 Inhibitor
HK2-IN-4 is a selective inhibitor of hexokinase 2 (HK2) with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. It disrupts the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1), leading to reduced lactate and ATP levels in cancer cells. Additionally, HK2-IN-4 promotes the activation of apoptosis pathways, evidenced by an increased p-AMPK/AMPK ratio and elevated Bax levels, alongside decreased Bcl2 levels. This compound is applicable in research focusing on colorectal cancer and non-small cell lung cancer, particularly in models with high HK2 expression. -
VDAC1 Inhibitor
AKOS-22 is a selective inhibitor of the mitochondrial protein VDAC1 (voltage-dependent anion channel 1), exhibiting an affinity with a Kd of 15.4 μM. This compound prevents VDAC1 oligomerization and inhibits apoptosis, thereby offering protection against mitochondrial dysfunction. AKOS-22 serves as a valuable tool in research focused on mitochondrial biology and related pathways in disease. -
VDAC1 Inhibitor
VBIT-3 is a selective inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization, exhibiting a binding affinity (Kd) of 31.3 μM. It functions as an apoptosis inhibitor, providing potential therapeutic applications in managing apoptosis-related disorders, including neurodegenerative and cardiovascular diseases. This reagent is valuable for research focused on understanding the biochemical pathways of apoptosis and exploring treatment strategies for related conditions. -
P-gp Inhibitor
P-gp Inhibitor 25 is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in drug transport and multidrug resistance. This compound enhances the oral bioavailability of paclitaxel, making it valuable in cancer therapy research. Its application in studies focused on overcoming P-gp-mediated drug resistance positions P-gp Inhibitor 25 as a significant tool in the development of effective anticancer treatments. -
P-gp Inhibitor
P-gp-IN-30 is a potent inhibitor of P-glycoprotein (P-gp) that acts by targeting Y-box binding protein 1 (YB-1). This compound enhances the sensitivity of cancer cells to Paclitaxel by decreasing both total and nuclear YB-1 protein levels, leading to the inhibition of P-gp expression and function, and consequently reducing the efflux of Paclitaxel. P-gp-IN-30 has demonstrated significant tumor growth inhibition in A549/Taxol xenograft mouse models and is applicable in research focused on non-small cell lung cancer (NSCLC). -
P-Glycoprotein Inhibitor
Reversin 205 is a selective inhibitor of P-glycoprotein (ABCB1), a crucial protein involved in drug transport and multidrug resistance. This compound serves as a peptide chemosensitizer, enhancing the efficacy of various chemotherapeutic agents by mitigating the efflux of drugs from cancer cells. Reversin 205 is applicable in research focused on overcoming drug resistance in cancer therapy and optimizing chemotherapy outcomes. -
P-glycoprotein Inhibitor
P-gp-IN-35 is a potent P-glycoprotein (P-gp) inhibitor, specifically designed to enhance the efficacy of chemotherapeutic agents. It demonstrates significant cytotoxic effects against breast and colorectal cancer cells, particularly in cases where P-gp is overexpressed, thus reversing multidrug resistance. This compound serves as a valuable tool in research focused on overcoming drug resistance in breast and colon cancers. -
P-glycoprotein Inhibitor
P-gp Inhibitor 5 is a selective inhibitor of P-glycoprotein (P-gp), a key player in multidrug resistance (MDR) in cancer. It exhibits notable antiproliferative activity against various cancer cell lines, effectively reinstating sensitivity to chemotherapeutic agents such as Vincristine and Paclitaxel in ABCB1/Flp-InTM-293 and KBvin cells. This property makes P-gp Inhibitor 5 a valuable tool for research aimed at overcoming drug resistance in cancer therapies. -
P-glycoprotein Inhibitor
KR30031 is a potent inhibitor of P-glycoprotein (P-gp), facilitating increased efficacy of anticancer drugs by overcoming multidrug resistance (MDR) pathways. This orally active compound is designed to enhance cytotoxic effects while minimizing cardiovascular side effects commonly associated with other P-gp inhibitors. KR30031 is valuable for research applications focused on understanding and reversing MDR in cancer therapeutic contexts. -
P-gp Inhibitor
P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that effectively reverses P-gp-mediated drug efflux. This 2,5-disubstituted furan derivative demonstrates significant affinity for P-gp through hydrogen bonding interactions with Asn 721 and Met 986. Its broad-spectrum reversal activity, coupled with low toxicity in MCF-7/ADR cell lines, makes P-gb-IN-1 a valuable tool for enhancing the efficacy of chemotherapeutic agents in research applications. -
P-glycoprotein Inhibitor
FM04 is a potent inhibitor of P-glycoprotein (P-gp) with an EC50 of 83 nM. It operates through two primary mechanisms: firstly, by binding to Q1193 and interacting with critical residues H1195 and T1226, and secondly, by engaging I1115, disrupting essential interactions within the R262-Q1081-Q1118 pocket, and uncoupling the ICL2-NBD2 interaction. FM04 is valuable for research exploring drug transport mechanisms and multidrug resistance in cancer therapies. -
P-gp Inhibitor
P-gp inhibitor 3 is a potent inhibitor of P-glycoprotein (P-gp), primarily targeting its ATPase activity to inhibit the efflux function. This compound demonstrates significant multidrug resistance (MDR) reversal capabilities, effectively enhancing the cytotoxic effects of antitumor agents such as Paclitaxel. P-gp inhibitor 3 is valuable in cancer research, particularly for studies focused on overcoming drug resistance in chemotherapy. -
P-gp Inhibitor
P-gp inhibitor 29 is a potent inhibitor of P-glycoprotein (P-gp) with an IC50 of 8.9 nM in Eca109/VCR cells. This compound not only inhibits P-gp activity but also induces apoptosis, making it a valuable tool in the study of drug resistance mechanisms in esophageal cancer. Its efficacy in modulating P-gp can facilitate research aimed at improving therapeutic strategies for this malignancy. -
P-gp Inhibitor
P-gp-IN-32 is a potent P-glycoprotein (P-gp) inhibitor that demonstrates significant ability to reverse multidrug resistance (MDR) in cancer cells. It exhibits low cytotoxicity with an IC50 of 0.11 μM and a reversal fold of 215.9 against Doxorubicin in MCF7/ADR cells. P-gp-IN-32 binds directly to P-gp, inducing conformational changes that inhibit its efflux function, making it a valuable tool for cancer research, particularly in studies focused on breast cancer. -
P-gp Inhibitor
P-gp Inhibitor 2 is a potent inhibitor of P-glycoprotein (P-gp), a critical transporter implicated in multidrug resistance. This compound effectively reverses Doxorubicin resistance with an IC50 of 0.22 µM in P-gp overexpressing human colorectal carcinoma SW600 Ad300 cells. Its application in cancer research highlights its potential as a valuable tool for overcoming P-gp-mediated drug efflux in therapeutic strategies. -
Pgp Inhibitor
P-gp inhibitor 15 is a nonsubstrate inhibitor targeting P-glycoprotein (P-gp), primarily acting to inhibit P-gp-ATPase activity. This compound effectively disrupts the P-gp-mediated efflux of Rhodamine123, leading to increased intracellular accumulation of chemotherapeutic agents. P-gp inhibitor 15 has demonstrated the ability to enhance the efficacy of Paclitaxel and shows potential in inhibiting tumor progression in xenograft models, specifically in nude mice with KBV tumors. -
P-glycoprotein Inhibitor
Dofequidar sesquifumarate is an orally active quinoline compound that functions as an inhibitor of P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). It exhibits a potent ability to reverse multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. This inhibition effectively blocks the efflux of chemotherapeutic agents, resulting in increased drug accumulation within cancer cells and enhanced chemotherapeutic efficacy. Dofequidar sesquifumarate is valuable for research applications aimed at overcoming drug resistance in cancer treatment. -
P-glycoprotein Inhibitor
(S)-Tenacissoside F is a polyoxypregnane compound that functions as a P-glycoprotein inhibitor. By effectively inhibiting the drug efflux activity of P-glycoprotein (P-gp/ABCB1), (S)-Tenacissoside F is capable of reversing multidrug resistance, making it a valuable compound in cancer research, particularly in the study of colon cancer. Its mechanism may provide insights into novel therapeutic approaches for overcoming drug resistance in tumors. -
P-gp Inhibitor
R 101933 is a potent inhibitor of P-glycoprotein (P-gp), a key mediator of drug efflux in cancer cells. By inhibiting P-gp, R 101933 enhances the intracellular accumulation of chemotherapeutic agents, making it valuable for studying drug resistance mechanisms in cancer research. This compound may also aid in identifying potential therapeutic strategies to improve the efficacy of anticancer drugs. -
MDR Inhibitor
Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp), targeting multidrug resistance (MDR) in cancer cells. This compound demonstrates significant reversal activity against MDR both in vitro and in vivo, likely due to its ability to inhibit P-gp overexpression and enhance intracellular accumulation of anticancer agents. As a brominated derivative of tetrandrine, Bromotetrandrine is a valuable reagent for evaluating MDR modulation in tumor research. -
Kv1.5 Inhibitor
MK-1832 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 86 nM. As a P-glycoprotein substrate, MK-1832 is particularly relevant for studying atrial fibrillation and related cardiovascular disorders. Its specificity for Kv1.5 makes it a valuable tool for investigating the molecular mechanisms underlying cardiac arrhythmias and for evaluating potential therapeutic interventions. -
P-gp Inhibitor
P-gp Inhibitor 26 is a potent inhibitor of P-glycoprotein (P-gp), a key player in multidrug resistance mechanisms. It effectively reverses P-gp-mediated drug resistance in K562/A02 cells, making it a valuable tool for investigating therapeutic strategies aimed at overcoming multidrug resistance in cancer cells. This compound is suitable for use in research applications focused on enhancing the efficacy of antitumor agents. -
P-gp Rransport Inhibitor
Phosphatidylinositol-1,2-dioctanoyl sodium acts as a potent inhibitor of P-glycoprotein (P-gp) transport. This compound demonstrates significant and reproducible inhibition of transmembrane P-gp transport, independent of cell line and substrate. Its involvement in signal transduction and cell motility makes it valuable for research into drug absorption and disposition, as well as studies on multidrug resistance in cancer therapy. -
P-gp Inhibitor
CJZ3 is a reversible inhibitor of P-glycoprotein (P-gp), which enhances the intracellular accumulation of the substrate drug Rh123. This compound is of particular interest in studies focused on improving drug permeability across the blood-brain barrier (BBB). CJZ3 has applications in research aimed at overcoming multidrug resistance and optimizing therapeutic efficacy for central nervous system-targeted therapies. -
P-glycoprotein Inhibitor
9,10-trans-Dehydroepothilone D is a potent P-glycoprotein inhibitor. It exhibits significant antiproliferative activity against paclitaxel-resistant cell lines that overexpress this transporter, making it a valuable tool in cancer research. Additionally, 9,10-trans-Dehydroepothilone D demonstrates tubulin polymerization activity, contributing to its potential use in elucidating mechanisms of drug resistance and improving therapeutic strategies. This compound serves as a promising candidate for further studies in cancer treatment paradigms. -
P-gp Inhibitor
Isotenulin acts as an inhibitor of P-glycoprotein (P-gp), enhancing the ATPase activity of P-gp and effectively combating multidrug resistance (MDR) in cancer cells. It demonstrates cytotoxic effects in both multidrug-resistant KB-vin cells and sensitive HeLaS3 cells. Additionally, Isotenulin shows a synergistic effect when used in conjunction with chemotherapeutic agents such as Paclitaxel, Vinblastine, and Doxorubicin, making it a valuable tool for research in cancer therapeutics. -
P-gp Inhibitor
8-Prenylchrysin is a C8-prenylated flavonoid that serves as a potent inhibitor of P-glycoprotein (P-gp). This compound demonstrates significant biological activity by modulating drug efflux, which can enhance the efficacy of chemotherapeutic agents. 8-Prenylchrysin is primarily utilized in cancer research to investigate its potential in overcoming multidrug resistance in tumor cells. -
P-glycoprotein Inhibitor
Encequidar hydrochloride is a potent P-glycoprotein (P-gp) inhibitor that enhances the oral bioavailability of P-gp substrate drugs. It exhibits exceptional potency with an IC50 of 0.63 nM, making it one of the most effective MDR1 inhibitors available. Encequidar significantly impedes the transepithelial transport of paclitaxel in MDCK monolayer cells, with an IC50 of 35.4 nM. This compound is valuable for research focused on pharmacokinetics and drug delivery systems. -
P-gp Inhibitor
Ardeemin, a P-glycoprotein inhibitor, effectively binds to and inhibits P-glycoprotein, thereby preventing the efflux of anticancer agents from cells. This mechanism helps to reverse the multidrug resistance phenotype in tumor cells, enhancing their sensitivity to chemotherapy. Ardeemin has demonstrated potential applications in cancer research, specifically in improving the efficacy of treatments for mammary carcinoma xenografts. -
P-glycoprotein Inhibitor
MS-073 (CP162398) is a potent inhibitor of P-glycoprotein (P-gp), a key transporter involved in multidrug resistance. By competitively inhibiting the binding of chemotherapeutic agents to P-glycoprotein, MS-073 effectively reverses resistance in drug-resistant cancer cells. This compound is valuable for research into overcoming therapeutic challenges in oncology and drug delivery. -
KV1.3 Inhibitor
KV1.3-IN-2 hydrochloride is a selective inhibitor of the KV1.3 potassium channel, with no impact on hERG channel activity. This compound is particularly valuable in the study of immune-related diseases, including psoriasis, rheumatoid arthritis, and systemic lupus erythematosus, due to its ability to modulate KV1.3-mediated cellular processes. Researchers can utilize KV1.3-IN-2 hydrochloride to explore mechanisms underlying these conditions and develop potential therapeutic strategies. -
Nav1.7 Inhibitor
Nav1.7-IN-19 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.49 μM. This compound exhibits significant selectivity for Nav1.7, with 312-fold and 662-fold selectivity over Nav1.1 and Nav1.5 in their inactivated states, respectively. Additionally, Nav1.7-IN-19 shows minimal inhibition of hERG potassium channels. Due to its analgesic properties, Nav1.7-IN-19 is valuable for research focused on neurological diseases. -
CPS1 Inhibitor
H3B-120 is a selective inhibitor of carbamoyl phosphate synthetase 1 (CPS1) that functions through competitive allosteric modulation, exhibiting an IC50 of 1.5 μM and a Ki of 1.4 μM. This compound demonstrates anti-cancer activity, making it a valuable tool for research into metabolic and oncological pathways. H3B-120 can be utilized in studies investigating the role of CPS1 in cancer metabolism and therapeutic targeting. -
Complex II Inhibitor
Atpenin A5 is a highly selective inhibitor of complex II, with an IC50 of approximately 10 nM. This compound acts as a potent mKATP channel agonist, offering cardioprotective effects. It is valuable for research applications focused on mitochondrial function, cardiac physiology, and energy metabolism. -
Kir6.2 Inhibitor
L-Palmitoylcarnitine chloride is a selective inhibitor of the Kir6.2 subunit of KATP channels. It disrupts membrane lipid homeostasis during ischemic conditions by accumulating in the sarcolemma while inhibiting channel activity without altering single-channel conductance. This compound is valuable for research into metabolic disturbances and the role of KATP channels in cardiac and skeletal muscle physiology. -
SK Channels Inhibitor
NS8593 hydrochloride is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels). This compound demonstrates reversible inhibition of SK3-mediated currents with a Kd value of 77 nM, as well as inhibiting SK1-3 subtypes in a Ca2+-dependent manner (Kds of 0.42, 0.60, and 0.73 μM respectively at 0.5 μM Ca2+). Importantly, NS8593 hydrochloride does not affect intermediate and large conductance Ca2+-activated K+ channels, such as hIK and hBK channels. It is valuable for research applications exploring the role of SK channels in cellular signaling and excitability. -
TMEM175 Inhibitor
AP-6 is a selective inhibitor of TMEM175, targeting lysosomal function modulation. This compound enhances lysosomal macromolecular catabolism, promoting accelerated digestive processes in macrophages and other cell types. AP-6 is a valuable tool in research related to Parkinson's disease, providing insights into lysosomal dysregulation and its implications in neurodegeneration.
