Chemical Structure : RJG-2051
CAS No.:
2851993-77-4
RJG-2051
(RJG2051)
Catalog No.: PC-24479Not For Human Use, Lab Use Only.
RJG-2051 is a potent, selective and covalent aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with IC50 of 13 nM, shows clear selectivity against AKR1C1 (2350-fold), AKR1C2 (1790-fold), and AKR1C4 (429-fold).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
RJG-2051 is a potent, selective and covalent aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with IC50 of 13 nM, shows clear selectivity against AKR1C1 (2350-fold), AKR1C2 (1790-fold), and AKR1C4 (429-fold).
RJG-2051 exhibits proteome-wide selectivity, shows negligible cross-reactivity with AKRs or other proteins across 1800+ tyrosine and lysine sites quantified by chemical proteomics.
RJG-2051 engages a noncatalytic tyrosine site (Y24).
RJG-2051 has IC50 of 27 nM in Coumberone reduction assays.
Physicochemical Properties
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M.Wt
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509.63
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Formula
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C26H31N5O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(4-((3-Cyclohexyl-1H-1,2,4-triazol-1-yl)sulfonyl)phenyl)(4-(2-methoxyphenyl)piperazin-1-yl)methanone
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References
1. Grams RJ, et al. J Med Chem. 2025 Apr 25. doi: 10.1021/acs.jmedchem.5c00050.
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