Catalog No.
Product Name
Application
Product Information
Citations
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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 Modulator
P-gp inhibitor 4 is a selective modulator of P-glycoprotein, exhibiting an EC50 of 94 nM. This compound enhances the transport of therapeutic agents across the gastrointestinal barrier and can restore the efficacy of doxorubicin in multidrug-resistant cancer cells. It serves as a valuable tool for research into overcoming drug resistance and improving drug delivery mechanisms. -
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-glycoprotein MDR Modulator
XR9051 is a specific modulator of P-glycoprotein, targeting multidrug resistance (MDR). This compound enhances the efficacy of chemotherapeutic agents by inhibiting P-glycoprotein activity, thereby improving drug accumulation in resistant cancer cells. XR9051 is primarily utilized in cancer research to investigate strategies for overcoming drug resistance and enhancing therapeutic outcomes. -
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. -
Natural Compound
Jatrophane 5 is a natural compound derived from Jatropha carcas L., targeting P-glycoprotein (P-gp). It exhibits potent inhibitory activity against P-gp, surpassing that of R(+)-verapamil and Tariquidar in colorectal multi-drug resistant DLD1-TxR cells. This compound is valuable for research into overcoming multidrug resistance in cancer treatment and enhancing drug efficacy in resistant cell types. -
Thiosemicarbazone
NSC73306 is a thiosemicarbazone that acts as a cell-penetrating cytotoxic agent. It demonstrates heightened toxicity in cells that express functional P-glycoprotein (P-gp) compared to non-expressing cells. This compound is primarily utilized in research focused on drug resistance mechanisms and potential therapeutic strategies against multidrug-resistant cancers. -
M1 Positive Allosteric Modulator, P-gp Substrate
VU6007477 is a selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM, notable for its ability to penetrate the blood-brain barrier. This compound also acts as a human P-glycoprotein (P-gp) substrate and exhibits moderate permeability, providing advantages in central nervous system (CNS) research. As a pyranyl amide derivative, VU6007477 is a valuable tool for investigating cholinergic seizure activity and related neurological disorders. -
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. -
P-glycoprotein Agonist
MCI826 is a P-glycoprotein (P-gp) agonist that enhances the efflux of various substrates across cell membranes. Its primary biological activity focuses on modulating drug transport and influencing cellular drug accumulation. This compound is valuable in research applications related to pharmacokinetics, multidrug resistance, and therapeutic strategies involving P-gp. -
Piezo1 Channel Activator
Jedi2 is a selective activator of the Piezo1 ion channel, facilitating mechanotransduction in various physiological processes. It demonstrates a binding affinity (Kd) of 2770 μM for mouse Piezo1 proteins, enabling the study of Piezo1's role in cellular responses to mechanical stimuli. This compound is suitable for research applications investigating the physiological and pathological implications of Piezo1 activation in multiple biological systems. -
Piezo1 Agonist
Yaddle1 is a potent agonist of the mechano-activated ion channel Piezo1, exhibiting a half-maximal effective concentration (MEC50) of 0.40 μM. This compound effectively promotes Ca2+ influx in T cells, leading to significant T cell activation. Yaddle1 serves as a valuable tool in research applications focused on vaccine adjuvants and the modulation of immune responses. -
Piezo1 Agonist
Yoda2 (KC289) functions as a Piezo1 agonist with an EC50 of 150 nM, facilitating calcium ion elevation and nitric oxide-dependent relaxation. This compound induces vasodilation in mouse arterial and cavernous tissues. Additionally, Yoda2 is implicated in inhibiting glucocorticoid-induced osteoclast formation and bone resorptive activity, effectively reversing glucocorticoid-mediated bone density loss and structural deterioration. Its applications extend to research in areas such as hypertension and osteoporosis. -
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. -
KCNQ2/3 Activator
Azetukalner is a selective Kv7.2/Kv7.3 potassium channel activator, demonstrating an EC50 of 27 nM. This compound exhibits approximately four-fold selectivity for the Kv7.2/7.3 combination over Kv7.3/7.5 and Kv7.4 channels, with EC50 values of 94 nM and 113 nM, respectively. Azetukalner's specificity exceeds 100-fold for Kv7 channels when compared to other ion channels and receptors. This reagent is valuable for research focused on focal epilepsy. -
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. -
TMEM175 Blocker
2-PPA is a selective blocker of the TMEM175 lysosomal potassium and proton channel, inhibiting the pore to occlude ion permeation pathways. This compound enhances lysosomal macromolecule degradation and accelerates macropinocytosis, making it a valuable tool in cellular and molecular research. 2-PPA's ability to covalently bind to hepatic proteins further supports its potential in investigating cellular processes. Its applications extend to the study of Parkinson's disease, providing insights into lysosomal function and related pathologies. -
ATP Analog
AMP-PNP tetralithium is a non-hydrolyzable ATP analog that serves as a potent inhibitor of ATP-dependent processes. It binds to ATP-binding sites without undergoing hydrolysis, thereby maintaining stable experimental conditions for the investigation of various biochemical pathways. This reagent is particularly valuable in studies of enzyme activity, kinase regulation, DNA and RNA metabolism, ion channel function, and protein complex assembly. -
Potassium Channel Activator
Pinacidil is a potent activator of ATP-sensitive potassium channels, primarily functioning as an antihypertensive agent. By facilitating K+ efflux in vascular smooth muscle, it induces hyperpolarization and promotes vasorelaxation, thereby inhibiting spontaneous tone and reducing contractions induced by agonists. Pinacidil is valuable for research applications in the study of cardiovascular diseases and vascular function. -
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. -
KCNQ2/Q3 Opener
ICA-27243 is a selective and orally active opener of the KCNQ2/Q3 potassium channels, exhibiting an EC50 of 0.38 μM. This compound has demonstrated potent antiepileptic and anticonvulsant properties, making it valuable for neurological research. Additionally, it shows lower efficacy towards KCNQ4 and the KCNQ3/Q5 channels, highlighting its specificity. ICA-27243 is an important tool for investigating the role of KCNQ channels in neuronal excitability and related disorders. -
KCC2 Activator
CLP257 is a selective activator of the K+-Cl cotransporter KCC2, exhibiting an EC50 of 616 nM. It specifically enhances Cl transport in neurons with reduced KCC2 activity while showing no effects on NKCC1, GABAA receptors, KCC1, KCC3, or KCC4. This compound is shown to alleviate hypersensitivity in neuropathic pain models in rats and modulates KCC2 protein turnover at the plasmalemmal level post-translationally. CLP257 is valuable for research into neuron excitability and synaptic transmission. -
Antiarrhythmic Agent
Flecainide is an orally active antiarrhythmic agent that primarily targets sodium channels to modulate cardiac excitability. By inhibiting calcium ion release mediated by the ryanodine receptor (RyR2), it plays a critical role in the study of arrhythmias. Research applications include the investigation of diseases such as catecholaminergic polymorphic ventricular tachycardia (CPVT), where it may help elucidate underlying mechanisms and therapeutic strategies. -
Ca2+-activated K+ Channel Inhibitor
Iberiotoxin is a potent inhibitor of Ca2+-activated K+ channels, derived from the venom of the Buthus tamulus scorpion. It demonstrates high specificity and selectivity, with an affinity (Kd) of approximately 1 nM, effectively blocking high conductance channels without affecting other voltage-dependent ion channels. This characteristic makes Iberiotoxin a valuable tool for investigating the physiological roles of Ca2+-activated K+ channels in various biological processes and for exploring their relevance in neurophysiological and cardiological research applications. -
TREK-1/2 Opener
BL-1249 is a selective opener of the TREK-1 (K2P2.1) and TREK-2 (K2P10.1) potassium channels, demonstrating potent activation with EC50 values of 5.5 μM and 8.0 μM, respectively. This compound effectively activates all members of the TREK subfamily while exhibiting no activity towards other K2P subfamilies. Notably, BL-1249 shows enhanced selectivity for bladder tissue, with an EC50 of 1.26 μM, compared to a higher EC50 of 21.0 μM in vascular tissue. The compound is valuable in research related to pain management and bladder function regulation. -
Kv12.2 (KCNH3) Inhibitor
ASP2905 is a potent inhibitor of the potassium channel Kv12.2 (KCNH3), encoded by the Kcnh3/BEC1 gene. This compound is orally active and capable of crossing the blood-brain barrier, exhibiting significant antipsychotic properties. ASP2905 is valuable for studying the roles of Kv12.2 in neuropsychiatric disorders and exploring therapeutic avenues for conditions such as schizophrenia. -
CHI3L1 Inhibitor
CHI3L1-IN-1 is a selective inhibitor of Chitinase-3-like protein 1 (CHI3L1), also known as YKL-40, with an IC50 of 50 nM. This compound exhibits additional effects by inhibiting the hERG channel with an IC50 of 2.3 μM. CHI3L1-IN-1 is valuable for research applications focused on the roles of CHI3L1 in inflammation and cancer, offering insights into its potential as a biomarker and therapeutic target. -
M-type K+ current Inhibitor
Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology. -
REK-1/TRAAK Agonist
2,2,2-Trichloroethanol functions as an agonist for the K2P potassium channels TREK-1 (KCNK2) and TRAAK (KCNK4). This compound is known to modulate neuronal excitability and plays a significant role in research related to pain, mood disorders, and neuroprotection. Its ability to enhance K2P channel activity makes it a valuable reagent for investigating the physiological and pharmacological properties of these ion channels. -
GIRK1/2 Activator
ML 297 is a potent and selective activator of GIRK1/2 channels, exhibiting an EC50 of 0.16 μM. This compound effectively crosses the blood-brain barrier, demonstrated by a brain-to-plasma ratio of 0.2 in murine models following intraperitoneal administration. ML 297 is under investigation for its potential therapeutic applications in the treatment of epilepsy. -
Potassium Channel Opener
Rimtuzalcap is a selective positive allosteric modulator targeting small-conductance calcium-activated potassium channels (SK channels). This compound exhibits key biological activity as a potassium channel opener, which may facilitate neuronal hyperpolarization and reduce excitability. Rimtuzalcap is primarily utilized in research focused on movement disorders, such as essential tremor (ET) and spinocerebellar ataxia (SCA), providing insights into potential therapeutic avenues for these conditions. -
Cationic Amphiphilic Lytic Peptide
L17E is an attenuated cationic amphiphilic lytic peptide that facilitates the delivery of macromolecules, including proteins, antibodies, and DNA nanostructures. Its mechanism involves membrane insertion and cleavage via electrostatic interactions, promoting intracellular escape. The effectiveness of L17E is closely linked to the expression of KCNN4, encoding the calcium-activated potassium channel KCa3.1, and it enhances cellular uptake through the induction of micropinocytosis. Additionally, L17E can be optimized through dimerization and combined with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles, for improved performance in research applications. -
KCNQ Channel Blocker
XE991 is a potent blocker of KCNQ (Kv7) channels, effectively inhibiting Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.3 (KCNQ3), and the M-current with IC50 values of 0.75 µM, 0.71 µM, 0.6 µM, and 0.98 µM, respectively. This selective inhibition makes XE991 a valuable tool for studying the physiological and pathophysiological roles of KCNQ channels in cells. It has applications in neurological research and the exploration of conditions related to ion channel dysfunction. -
Kv1.3 Inhibitor
Margatoxin is a highly selective inhibitor of the voltage-gated potassium channel Kv1.3, with a binding affinity (Kd) of 11.7 pM. It also exhibits inhibitory effects on Kv1.2 (Kd = 6.4 pM) and Kv1.1 (Kd = 4.2 nM). This 39-amino-acid peptide, derived from the venom of Centruroides margaritatus, is extensively utilized in ion channel research to study the role of Kv1.3 in various physiological and pathophysiological processes. -
KATP Channel Blocker
5-Hydroxydecanoate sodium is a selective blocker of ATP-sensitive K+ (KATP) channels, exhibiting an IC50 of approximately 30 μM. This compound serves as a substrate for mitochondrial outer membrane acyl-CoA synthetase and possesses antioxidant properties. It is primarily utilized in research to study the physiological and pathophysiological roles of KATP channels in various cellular processes. -
KCNQ1/mink Activator
L-364,373 is a selective activator of the voltage-gated Kv7.1 (KCNQ1) channels. It enhances the Iks (slow delayed rectifier potassium current) and significantly shortens action potential duration in guinea pig cardiac myocytes, while also suppressing early afterdepolarizations in rabbit ventricular myocytes. This compound is valuable for research on cardiac electrophysiology and the mechanisms underlying cardiac arrhythmias. -
hERG Channel Activator
ICA-105574 is a potent hERG channel activator that primarily functions by inhibiting the inactivation of hERG channels. It significantly increases current amplitudes by more than 10-fold, demonstrating an EC50 of 0.5 ± 0.1 μM and a Hill slope of 3.3 ± 0.2. This compound has been shown to prevent arrhythmias resulting from cardiac delayed repolarization and can concentration-dependently shorten action potential duration in ventricular myocytes, making it valuable for cardiovascular research applications. -
Kv1.3 Inhibitor
Dalazatide is a potent inhibitor of the Kv1.3 potassium channel, specifically designed for research applications in autoimmune diseases. This peptide has shown efficacy in the modulation of immune responses, making it a valuable tool for studying conditions such as multiple sclerosis, lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease. Its role in Kv1.3 inhibition provides insights into the pathophysiology of these diseases and potential therapeutic avenues. -
Kv7.2/7.3 Activator
Opakalim is a selective activator of Kv7.2 and Kv7.3 potassium channels, exhibiting an EC50 of 0.6 μM. It demonstrates minimal activation of GABAA receptors while offering potent anti-seizure efficacy in the maximal electroshock seizure (MES) model. Opakalim is suitable for research applications focused on seizure mechanisms and the modulation of neuronal excitability. -
Anti-arrhythmic Agent
Ibutilide is a potent anti-arrhythmic agent primarily targeting the rapidly activating delayed rectifier K+ current (IKr). By prolonging action potentials, it effectively manages cardiac arrhythmias. This compound is commonly utilized in electrophysiology research to study cardiac action potentials and the mechanisms underlying arrhythmogenesis.
