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AKR1C3 inhibitor SG-55

Chemical Structure : AKR1C3 inhibitor SG-55

CAS No.:

AKR1C3 inhibitor SG-55

Catalog No.: PC-26001Not For Human Use, Lab Use Only.

AKR1C3 inhibitor SG-55 is a potent, selective and noncompetitive aldo-keto reductase 1C3 (AKR1C3) inhibitor with IC50 of 5 nM, with no inhibition against AKR1C1, AKR1C2, and AKR1C4.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AKR1C3 inhibitor SG-55 is a potent, selective and noncompetitive aldo-keto reductase 1C3 (AKR1C3) inhibitor with IC50 of 5 nM, with no inhibition against AKR1C1, AKR1C2, and AKR1C4.
SG-55 elevated the reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP+) ratio, decreased the reduced/oxidized glutathione (GSH/GSSG) ratio, induced DNA double-strand breaks.
SG-55 synergized with Osimertinib to suppress proliferation, clonogenicity, and survival in 19Del/T790M/C797S mutant NSCLC cells.
SG-55 demonstrated efficacy in xenograft models and exhibited favorable pharmacokinetics in mice.

Physicochemical Properties

M.Wt 319.36
Formula C19H17N3O2
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

2-{[4-(Cyclopropylcarbonyl)-1H-Pyrrol-2-yl]carbonyl}-1,2,3,4-Tetrahydroisoquinoline-7-Carbonitrile

References

1. Can Guo, et al. J Med Chem. 2026 Jan 29. doi: 10.1021/acs.jmedchem.5c03655.

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