| S1603 |
Furosemide
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Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.
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J Immunother Cancer, 2024, 12(11)e009805
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bioRxiv, 2023, 2023.07.12.548707
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Ren Fail, 2022, 44(1):1345-1355
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| S1287 |
Bumetanide
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Bumetanide is a loop diuretic of the sulfamyl category to treat heart failure. This compound is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
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Journal of Cellular Physiology, February 2019, 1630-1642
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J Immunother Cancer, 2024, 12(11)e009805
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PLoS Pathog, 2024, 20(10):e1012601
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| S5194 |
Furosemide sodium
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Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.
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Nat Commun, 2024, 15(1):7342
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Ren Fail, 2022, 44(1):1345-1355
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| E2358 |
Azosemide
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Azosemide is a potent Na+–K+–2Cl− cotransporter NKCC1 inhibitor with IC50s of 0.246 µM for hNKCC1A and 0.197 µM for NKCC1B, respectively.
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| E6462New |
IAMA-6
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IAMA‑6 (ARN23746) is a potent, selective, and orally bioavailable inhibitor of the NKCC1 cotransporter. It exhibits the potential to be primarily used in research to treat cognitive impairment in Down syndrome and autism by regulating intracellular chloride homeostasis.
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| S8615 |
Sodium Dichloroacetate (DCA)
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DCA (Sodium dichloroacetate), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
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bioRxiv, 2025, 2025.04.03.647023
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bioRxiv, 2025, 2025.08.24.671623
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bioRxiv, 2025, 2023.08.11.552890
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