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KVS0001

Chemical Structure : KVS0001

CAS No.:

KVS0001 (KVS 0001, KVS-0001)

Catalog No.: PC-21705Not For Human Use, Lab Use Only.

KVS0001 is a specific and bioavailable small molecule inhibitor of SMG1 kinase, disrupts nonsense mediated decay (NMD).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KVS0001 is a specific and bioavailable small molecule inhibitor of SMG1 kinase, disrupts nonsense mediated decay (NMD).
KVS0001 is highly selective against the other 246 protein or lipid kinases up to 1 uM.
KVS0001 substantially decreases the amount of phosphorylated UPF1, the downstream target of SMG1 kinase activity in NCI-H358 and LS180 cells.
KVS0001 causes MHC class I display of hidden neoantigens, increases the expression of TP53 in cancer cell lines, NCI-H716 and NCI-H2228.
KVS0001 (30 mg/kg) impacts tumor growth in syngeneic models.
KVS0001 elevates the expression of transcripts and proteins resulting from truncating mutations in vivo and in vitro.

Physicochemical Properties

M.Wt 579.08
Formula C27H27ClN8O3S
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

1-(4-(4-(2-((4-chloro-3-(piperazin-1-ylsulfonyl)phenyl)amino)pyrimidin-4-yl)pyridin-2-yl)phenyl)-3-methylurea

References

1. Ashley L Cook, et al. bioRxiv. 2023 Dec 29:2023.12.28.573594.

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