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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Aldose Reductase-RJG-2051
RJG-2051

Chemical Structure : RJG-2051

CAS No.: 2851993-77-4

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RJG-2051 (RJG2051)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 509.63
分子式 C26H31N5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(4-((3-Cyclohexyl-1H-1,2,4-triazol-1-yl)sulfonyl)phenyl)(4-(2-methoxyphenyl)piperazin-1-yl)methanone

参考文献

1. Grams RJ, et al. J Med Chem. 2025 Apr 25. doi: 10.1021/acs.jmedchem.5c00050.

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