| Cas No.: | 2123489-30-3 |
| Chemical Name: | (5-Chloro-2-(2-(methylamino)thiazol-4-yl)pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone |
| Synonyms: | WNK-IN-11; WNK IN 11; WNKIN11; WNK inhibitor 11; WNK inhibitor-11,2123489-30-3 |
| SMILES: | O=C(C1=CC(C2=CSC(NC)=N2)=NC=C1Cl)N3CCN(CC4=CC=C(Cl)C=C4)CC3 |
| Formula: | C21H21Cl2N5Os |
| M.Wt: | 462.39 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1. |
| Target: | IC50: 4 nM (WNK1)[1]. |
| In Vitro: | WNK-IN-11 (compound 11) shows IC50<2 μM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility, albeit with still rather high microsomal clearance. WNK-IN-11 shows ATP noncompetitive inhibition. When tested against a panel of 440 human kinases at 10 μM concentration, 2500-fold above enzyme IC50 value, WNK-IN-11 shows excellent selectivity with only a few significant off-target kinase inhibitions, most notably BTK and feline encephalitis virus-related (FER) kinase, neither of which are implicated for blood pressure regulation. This excellent selectivity profile is consistent with the predicted allosteric binding mode outside the highly conserved ATP-pocket[1]. |
| References: | [1]. Yamada K, et al. Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models. J Med Chem. 2017 Aug 24;60(16):7099-7107. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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