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SARS-CoV-2 nsp12 NiRAN domain inhibitor NCI-2

Chemical Structure : SARS-CoV-2 nsp12 NiRAN domain inhibitor NCI-2

CAS No.:

SARS-CoV-2 nsp12 NiRAN domain inhibitor NCI-2 (SW090466, NiRAN covalent inhibitor 2)

Catalog No.: PC-23595Not For Human Use, Lab Use Only.

NCI-2 is a small molecule inhibitor of SARS-CoV-2 nsp12 NiRAN domain, covalently binds to an active site cysteine (Cys53) in the NiRAN domain, inhibiting nsp12-dependent AMPylation of nsp9 with IC50 of 4.3 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

NCI-2 is a small molecule inhibitor of SARS-CoV-2 nsp12 NiRAN domain, covalently binds to an active site cysteine (Cys53) in the NiRAN domain, inhibiting nsp12-dependent AMPylation of nsp9 with IC50 of 4.3 uM.
NCI-2 can enter cells, bind to, and inactivate ectopically expressed nsp12.
NCI-2 shows inhibition of NiRAN-dependent RNAylation of nsp9 and an increase in the thermal stability of nsp12.
NCI-2 demonstrates limited potency in inhibiting SARS-CoV-2 replication (IC50=200 uM).

Physicochemical Properties

M.Wt 240.64
Formula C10H9ClN2O3
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

methyl 5-(chloromethyl)-7-hydroxypyrazolo[1,5-a]pyridine-3-carboxylate

References

1. Hernandez G, et al. bioRxiv [Preprint]. 2024 Nov 25:2024.11.22.624893.

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