S8279 |
Shikonin
|
Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
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Elife, 2024, 12RP91141
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Elife, 2024, 12RP91141
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Mol Ther Methods Clin Dev, 2024, 32(3):101307
|
|
S1351 |
Ivermectin
|
Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
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J Clin Invest, 2024, 134(22)e181314
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Viruses, 2024, 16(4)640
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Life Sci Alliance, 2023, 6(8)e202302133
|
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S1698 |
Torsemide
|
Torsemide (AC-4464, JDL-464) is a pyridyl sulfonylurea with a chemical structure between that of traditional loop diuretics and Cl- channel blockers, used to treat hypertension. |
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J Immunother Cancer, 2024, 12(11)e009805
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Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
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S0454 |
Adjudin
|
Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation. |
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Brain Res Bull, 2022, 182:80-89
|
|
S1675 |
Lubiprostone
|
Lubiprostone (RU 0211,SPI-0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation. |
|
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S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0125 |
CaCCinh-A01
|
CaCCinh-A01 (TMEM16 Blocker I) is a blocker of TMEM16A with IC50 of 2.1 μM. CaCCinh-A01 is also an inhibitor of calcium-activated chloride channel (CaCC) with IC50 of ~ 10 μM. |
|
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A2726 |
Anti-ANO1 / TMEM16A
|
Anti-ANO1 / TMEM16A is a humanized monoclonal antibody that binds to human TMEM16A and modulates its activity, with potential anti-tumor activity. MW: 146.8 KD. |
|
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S4339 |
Meticrane
|
Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension. |
|
|
S3807 |
Dehydroandrographolide
|
Dehydroandrographolide, isolated from Andrographis paniculata (Burm. F.) Nees (Chuan-xin-lian), is a novel TMEM16A inhibitor and possesses multiple pharmacological activities, including anti-inflammation, anti-cancer, anti-bacterial, anti-virus and anti-hepatitis activity. |
|
|
S6439 |
Talniflumate
|
Talniflumate (MSI-1995) is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma. Talniflumate is also an inhibitor of human calcium-activated chloride channels. |
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Acta Pharm Sin B, 2023, 13(2):662-677
|
|
S2955 |
NS1652
|
NS1652 is a reversible chloride channel blocker, potently inhibits the chloride conductance (IC50 = 1.6 μM) in human and mouse red blood cells, but only weakly volume activated anion conductance (VRAC) (IC50 = 125 μM) in HEK293 cells. |
|
|
S6470 |
Fluralaner
|
Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls). |
|
|
S1203 |
T16Ainh-A01
|
T16Ainh-A01 is a potent and selective inhibitor of calcium-activated chloride channel (CaCC)/transmembrane protein 16A (TMEM16A, ANO1) with IC50 of 1.8 μM.
|
|
|
S8279 |
Shikonin
|
Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
- Elife, 2024, 12RP91141
- Elife, 2024, 12RP91141
- Mol Ther Methods Clin Dev, 2024, 32(3):101307
|
|
S1698 |
Torsemide
|
Torsemide (AC-4464, JDL-464) is a pyridyl sulfonylurea with a chemical structure between that of traditional loop diuretics and Cl- channel blockers, used to treat hypertension. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
|
S0454 |
Adjudin
|
Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation. |
- Brain Res Bull, 2022, 182:80-89
|
|
S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0125 |
CaCCinh-A01
|
CaCCinh-A01 (TMEM16 Blocker I) is a blocker of TMEM16A with IC50 of 2.1 μM. CaCCinh-A01 is also an inhibitor of calcium-activated chloride channel (CaCC) with IC50 of ~ 10 μM. |
|
|
S4339 |
Meticrane
|
Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension. |
|
|
S3807 |
Dehydroandrographolide
|
Dehydroandrographolide, isolated from Andrographis paniculata (Burm. F.) Nees (Chuan-xin-lian), is a novel TMEM16A inhibitor and possesses multiple pharmacological activities, including anti-inflammation, anti-cancer, anti-bacterial, anti-virus and anti-hepatitis activity. |
|
|
S6439 |
Talniflumate
|
Talniflumate (MSI-1995) is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma. Talniflumate is also an inhibitor of human calcium-activated chloride channels. |
- Acta Pharm Sin B, 2023, 13(2):662-677
|
|
S2955 |
NS1652
|
NS1652 is a reversible chloride channel blocker, potently inhibits the chloride conductance (IC50 = 1.6 μM) in human and mouse red blood cells, but only weakly volume activated anion conductance (VRAC) (IC50 = 125 μM) in HEK293 cells. |
|
|
S6470 |
Fluralaner
|
Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls). |
|
|
S1203 |
T16Ainh-A01
|
T16Ainh-A01 is a potent and selective inhibitor of calcium-activated chloride channel (CaCC)/transmembrane protein 16A (TMEM16A, ANO1) with IC50 of 1.8 μM.
|
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