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Chemical Structure : ZT-1a
CAS No.: 212135-62-1
Catalog No.: PC-72593Not For Human Use, Lab Use Only.
ZT-1a (STK39 inhibitor ZT-1a, SPAK-IN-ZT-1a) is a novel potent, selective SPAK kinase (STK39) inhibitor.
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ZT-1a (STK39 inhibitor ZT-1a, SPAK-IN-ZT-1a) is a novel potent, selective SPAK kinase (STK39) inhibitor.
ZT-1a potently inhibited SLC12A cation-Cl-cotransporters (CCC), phosphorylation of NKCC1 p-Thr203/207/212 by 72% at 1uM and phosphorylation of KCC sites 1/2 by 65-77% at 3 uM in HEK-293 cells.
ZT-1a is a more potent modulator of SPAK-dependent CCC phosphorylation than the current SPAK kinase inhibitors Closantel, STOCK1S-50699, and STOCK1S-14279.
ZT-1a inhibited SPAK phosphorylation at Ser373 in HEK-293 cells (70% inhibition at 3-10 uM).
ZT-1a disrupts SPAK interaction with WNK but not with MO25α, reduces SPAK-dependent CCC phosphorylation in cells, inhibits NKCC1 but stimulates KCC3 activity.
ZT-1a decreases SPAK-CCC phosphorylation in hemorrhagic hydrocephalus, modulates primary cortical neuron volume, reduces stroke-associated cerebral edema and infarct, improves neurological function after ischemic stroke in vivo.
| M.Wt | 445.73 | |
| Formula | C22H15Cl3N2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-chloro-N-(5-chloro-4-((4-chlorophenyl)(cyano)methyl)-2-methylphenyl)-2-hydroxybenzamide |
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1. Jinwei Zhang, et al. Nat Commun. 2020 Jan 7;11(1):78.
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