G12Si-1
G12Si-1 is a selective K-Ras (G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras (G12S) . G12Si-1 shows good ability to covalently engage recombinant K-Ras (G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange[1].
Product Specifications
CAS Number
[2946593-42-4]
UNSPSC
12352005
Target
Ras
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/g12si-1.html
Solubility
10 mM in DMSO
Smiles
ClC1=CC=CC2=CC=CC(N3CC4=C(CC3)C(N5CC(C6CC5)OC6=O)=NC(OC[C@@H]7CCCN7C)=N4)=C21
Molecular Formula
C29H32ClN5O3
Molecular Weight
534.05
References & Citations
[1]Zhang Z, et al. Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras (G12S) . Nat Chem Biol. 2022 Jul 21.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
K-Ras
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