Potassium Channel

Inhibitory Selectivity

Potassium Channel Products

All (38) Potassium Channel Inhibitors (24) Potassium Channel Activators (10) Potassium Channel Agonists (1) Potassium Channel Modulators (2) Potassium Channel Chemicals (1) New Potassium Channel Products

Catalog No.	Information	Product Use Citations
S2825	ML133 HCl ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.	Nat Commun, 2022, 13(1):3544 Cell Mol Immunol, 2022, 19(8):925-943 Mol Pain, 2019, 15:1744806919838947
S4489	Tetraethylammonium chloride Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.
S4495	Quinine Quinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM.	Cell Mol Immunol, 2022, 19(8):925-943 J Pharmacol Toxicol Methods, 2017, 90:39-47
S4681	Quinidine hydrochloride monohydrate Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.	J Biomed Res, 2021, 35(5):395-407
E0144^New	Vernakalant (RSD1235) Hydrochloride Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
E0015^New	Iberiotoxin Iberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM.
S9223	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S0524	A2793 A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.
S3242	Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the K_ATP current, influx of Ca²⁺ to the intracellular.
S0741	A2764 dihydrochloride A2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception.
S9251	Oxypeucedanin Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.
E0012	1-EBIO 1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone）is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.
E0001	DCPIB DCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM.
S0087	JNJ 303 JNJ 303 is a potent blocker of the voltage dependent I_Ks-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).
S0090	NS6180 NS-6180 is a highly selective inhibitor of KCa3.1 ion channel with IC50 value of 9 nM, which inhibits T cell activation and inflammation.
S6554	ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S2405	Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.	Int J Biol Sci, 2019, 15(11):2497-2508 Front Pharmacol, 2019, 10:1219 J Med Virol, 2019, 91(8):1440-1447
S0398	Astemizole Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S0188	GSK369796 Dihydrochloride GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.
S5773	NS1643 NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.
S4439	Almitrine mesylate Almitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca²⁺-dependent K⁺ channel by decreasing its open probability with IC50 of 0.22 μM.
S0476	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S2967	XE991 dihydrochloride XE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.
S6627	E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.
S6978^New	VU0071063 VU0071063 activates heterologously expressed Kir6.2/SUR1 channels with a EC50 of 7 μM, dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca²⁺ entry and insulin secretion.
S0050	ML277 ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.
S0311	SKA-31 SKA-31(Naphtho[1,2-d]thiazol-2-ylamine) is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively.
S6559	ML-297 ML-297 (VU 0456810, CID 56642816) is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.
S6553	ML213 ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively.
S0144	ICA 069673 ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.
S6572	ML335 ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
E0030	NS309 NS309 is a potent and selective activator of human Ca²⁺ -activated K⁺ channels of SK and IK types with an EC50 of 150 nM for hSK3 channel, and displays no activity at BK channels.
S0462	NS-1619 NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.
S0467	Emodepside Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.
E0105^New	ICA-27243 ICA-27243, a selective activator of the neuronal M current and KCNQ2/Q3 channels, induces a concentration-dependent increase in a ⁸⁶Rb⁺ efflux from CHO cells expressing KCNQ2/Q3 channels with EC50 of 0.2 μM.
E0034^New	CyPPA CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels.
S0075	ICA-110381 ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.
S6653	Nigericin (NSC 292567) sodium salt Nigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H⁺, K⁺, and Pb²⁺ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes.	J Hazard Mater, 2022, 436:129093 Biomed Pharmacother, 2022, 150:112978 J Virol, 2022, 96(14):e0212721

Catalog No.	Information	Product Use Citations
S2825	ML133 HCl ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.	Nat Commun, 2022, 13(1):3544 Cell Mol Immunol, 2022, 19(8):925-943 Mol Pain, 2019, 15:1744806919838947
S4489	Tetraethylammonium chloride Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.
S4495	Quinine Quinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM.	Cell Mol Immunol, 2022, 19(8):925-943 J Pharmacol Toxicol Methods, 2017, 90:39-47
S4681	Quinidine hydrochloride monohydrate Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.	J Biomed Res, 2021, 35(5):395-407
E0144^New	Vernakalant (RSD1235) Hydrochloride Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
E0015^New	Iberiotoxin Iberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM.
S9223	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S0524	A2793 A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.
S3242	Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the K_ATP current, influx of Ca²⁺ to the intracellular.
S0741	A2764 dihydrochloride A2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception.
S9251	Oxypeucedanin Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.
E0012	1-EBIO 1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone）is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.
E0001	DCPIB DCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM.
S0087	JNJ 303 JNJ 303 is a potent blocker of the voltage dependent I_Ks-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).
S0090	NS6180 NS-6180 is a highly selective inhibitor of KCa3.1 ion channel with IC50 value of 9 nM, which inhibits T cell activation and inflammation.
S6554	ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S2405	Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.	Int J Biol Sci, 2019, 15(11):2497-2508 Front Pharmacol, 2019, 10:1219 J Med Virol, 2019, 91(8):1440-1447
S0398	Astemizole Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S0188	GSK369796 Dihydrochloride GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.
S5773	NS1643 NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.
S4439	Almitrine mesylate Almitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca²⁺-dependent K⁺ channel by decreasing its open probability with IC50 of 0.22 μM.
S0476	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S2967	XE991 dihydrochloride XE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.
S6627	E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.

Catalog No.	Information	Product Use Citations	Product Validations
S6978^New	VU0071063 VU0071063 activates heterologously expressed Kir6.2/SUR1 channels with a EC50 of 7 μM, dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca²⁺ entry and insulin secretion.
S0050	ML277 ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.
S0311	SKA-31 SKA-31(Naphtho[1,2-d]thiazol-2-ylamine) is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively.
S6559	ML-297 ML-297 (VU 0456810, CID 56642816) is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.
S6553	ML213 ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively.
S0144	ICA 069673 ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.
S6572	ML335 ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
E0030	NS309 NS309 is a potent and selective activator of human Ca²⁺ -activated K⁺ channels of SK and IK types with an EC50 of 150 nM for hSK3 channel, and displays no activity at BK channels.
S0462	NS-1619 NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.
S0467	Emodepside Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.

Catalog No.	Information	Product Use Citations	Product Validations
E0105^New	ICA-27243 ICA-27243, a selective activator of the neuronal M current and KCNQ2/Q3 channels, induces a concentration-dependent increase in a ⁸⁶Rb⁺ efflux from CHO cells expressing KCNQ2/Q3 channels with EC50 of 0.2 μM.

Catalog No.

Information

Product Use Citations

Product Validations

E0105^New

ICA-27243

ICA-27243, a selective activator of the neuronal M current and KCNQ2/Q3 channels, induces a concentration-dependent increase in a ⁸⁶Rb⁺ efflux from CHO cells expressing KCNQ2/Q3 channels with EC50 of 0.2 μM.

Catalog No.	Information	Product Use Citations	Product Validations
E0034^New	CyPPA CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels.
S0075	ICA-110381 ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

Catalog No.

Information

Product Use Citations

Product Validations

E0034^New

CyPPA

CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels.

S0075

ICA-110381

ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

Catalog No.	Information	Product Use Citations	Product Validations
S6653	Nigericin (NSC 292567) sodium salt Nigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H⁺, K⁺, and Pb²⁺ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes.	J Hazard Mater, 2022, 436:129093 Biomed Pharmacother, 2022, 150:112978 J Virol, 2022, 96(14):e0212721

Catalog No.

Information

Product Use Citations

Product Validations

S6653

Nigericin (NSC 292567) sodium salt

Nigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H⁺, K⁺, and Pb²⁺ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes.

J Hazard Mater, 2022, 436:129093

Biomed Pharmacother, 2022, 150:112978

J Virol, 2022, 96(14):e0212721

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