Stock solution can be stored below -20℃ for several months. For higher solubility, warming the tube at 37 ℃ and shaking it in the ultrasonic bath is recommended.
SML2809
WNK463
≥98% (HPLC)
Synonym(s):
N-(1,1-Dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-1H-imidazole-5-carboxamide, N-tert-Butyl-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-4-yl)-1H-imidazole-5-carboxamide
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About This Item
Empirical Formula (Hill Notation):
C21H24F3N7O2
CAS Number:
Molecular Weight:
463.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and availability is not currently available.
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
FC(F)(F)c1nnc([o]1)c2cnc(cc2)N3CCC(CC3)[n]4cncc4C(=O)NC(C)(C)C
InChI
1S/C21H24F3N7O2/c1-20(2,3)27-17(32)15-11-25-12-31(15)14-6-8-30(9-7-14)16-5-4-13(10-26-16)18-28-29-19(33-18)21(22,23)24/h4-5,10-12,14H,6-9H2,1-3H3,(H,27,32)
InChI key
HWSHOMMVLGBIDN-UHFFFAOYSA-N
Biochem/physiol Actions
Orally active, highly selective & potent ATP-competitive inhibitor against with-No-Lysine (K) kinases WNK1-4 with in vivo efficacy in rodent models of hypertension.
WNK463 is a high-affinity, ATP-competitive inhibitor against with-No-Lysine (K) kinases (hWNK1/3/4 IC50 = 5/6/9 nM with MBP & 1 μM ATP, hWNK2 IC50 = 1 nM with MBP & 2 μM ATP, hWNK1 IC50 = 41 nM with OSR1 & 0.5 μM ATP; hWNK1/4 KD = 3.71/3.84 by SPR), exhibiting weak affinity against only two other human kinases among a panel of 442. WNK463 downregulates the overexpressed OSR1 phosphorylation level in HEK293 cells (IC50 = 106 nM; 1 hr) and displays in vivo efficacy in rodent hypertension models (1-10 mg/kg in rats p.o., 10 mg/kg in hWNK1 transgenic mice p.o.) with good orally availability (F = 100%/mice & 74%/rats post 1.5 mg/kg p.o.).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Adam Volanakis et al.
Genes & development, 31(21), 2175-2185 (2017-12-03)
Nuclear gene transcription is coordinated with transcript release from the chromatin template and messenger RNA (mRNA) export to the cytoplasm. Here we describe the role of nuclear-localized kinase WNK1 (with no lysine [K] 1) in the mammalian mRNA export pathway
Melaine A Kuenemann et al.
Molecular informatics, 37(6-7), e1700138-e1700138 (2018-02-24)
The With-No-Lysine (WNK) serine/threonine kinase family constitutes a unique and distinctive branch of the kinome. The four proteins of this family (WNK1/2/3/4) are involved in blood pressure regulation, body fluid, and electrolyte homeostasis. Herein, we modeled and analyzed the binding
Ken Yamada et al.
Nature chemical biology, 12(11), 896-898 (2016-10-19)
The With-No-Lysine (K) (WNK) kinases play a critical role in blood pressure regulation and body fluid and electrolyte homeostasis. Herein, we introduce the first orally bioavailable pan-WNK-kinase inhibitor, WNK463, that exploits unique structural features of the WNK kinases for both
Clinton A Taylor et al.
Proceedings of the National Academy of Sciences of the United States of America, 115(15), 3840-3845 (2018-03-28)
The with-no-lysine (K) (WNK) signaling pathway to STE20/SPS1-related proline- and alanine-rich kinase (SPAK) and oxidative stress-responsive 1 (OSR1) kinase is an important mediator of cell volume and ion transport. SPAK and OSR1 associate with upstream kinases WNK 1-4, substrates, and
Jinwei Zhang et al.
Science signaling, 9(450), e3-e3 (2016-11-05)
The with-no-lysine (K) WNK kinases are master regulators of the Na+-(K+)-Cl- cotransporters, including the renal-specific NCC and NKCC2 cotransporters. The discovery of WNK463, an orally bioavailable pan-WNK kinase inhibitor that exploits unique structural properties of the WNK catalytic domain to
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