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Kv2.1-syntaxin inhibitor 15

Chemical Structure : Kv2.1-syntaxin inhibitor 15

CAS No.: 1203036-62-7

Kv2.1-syntaxin inhibitor 15 (Kv2.1-syntaxin-IN-15)

Catalog No.: PC-73038Not For Human Use, Lab Use Only.

Kv2.1-syntaxin inhibitor 15 (Kv2.1-syntaxin-IN-15, Cpd5) is a small molecule Kv2.1-syntaxin-binding inhibitor (IC50=5.5 uM) with neuroprotective properties.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Kv2.1-syntaxin inhibitor 15 (Kv2.1-syntaxin-IN-15, Cpd5) is a small molecule Kv2.1-syntaxin-binding inhibitor (IC50=5.5 uM) with neuroprotective properties.
Kv2.1-syntaxin inhibitor 15 competitively binds syntaxin against C1aB-containing Kv2.1 peptides with IC50 of 5.5 uM.
Kv2.1-syntaxin inhibitor 15 (10 uM) significantly diminished threo-β-benzyloxyaspartate (TBOA, 75 uM)-induced toxicity neuronal cultures, ameliorated significant cellular damage, by preventing the expression of enhanced Kv2.1-mediated K+ currents.
Kv2.1-syntaxin inhibitor 15 is a first-in-class inhibitor of Kv2.1 binding to Syntaxin, likely due to inhibition of the C1a region of Kv2.1 binding to syntaxin.
Cpd5 (10 μM) does not affect evoked AMPAR EPSCs in layer 2/3 corticocallosal neurons in the mouse auditory cortex.

Physicochemical Properties

M.Wt 419.499
Formula C23H21N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[3-(1,3-benzothiazol-2-yl)phenyl]-1-[(3,4-dimethoxyphenyl)methyl]urea

References

1. Yeh CY, et al. Proc Natl Acad Sci U S A. 2019 Jul 30;116(31):15696-15705.

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