RGNCY-0013 (Glucocorticoid Resistance Inhibitor)
This compound (J9) was selected for its lead-like properties at restoring sensitivity to glucocorticoid resistant T-ALL cells (CUTLL1 cell line) through the upregulation of the glucocorticoid receptor. Patients can develop glucocorticoid resistance rendering the treatment ineffective. J9 and its mechanism of action provides a useful strategy for overcoming this resistance. The EC50 of J9 in combination with dextramethasone is 28 uM.
Systematic Name: 4-cyclopropyl-5-(pyridin-4-yl)pyrimidin-2-amine
Molecular Weight: 212.26
- PMID: 25050160
Reference: Alexandra M. Cantley, Matthew Welsch, Alberto Ambesi-Impiombato, Marta Sanchez-Martin, Mi-Yeon Kim, Andras Bauer, Adolfo Ferrando, and Brent R. Stockwell. “Small Molecule that Reverses Dexamethasone Resistance in T-cell Acute Lymphoblastic Leukemia (T-ALL).” ACS Medicinal Chemistry Letters 5.7 (2014): 754-759
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Tags: RGNCY-0013, Gucocorticoid, J9, T-ALL, CUTLL1