CRT0083914
CAS No. : 932495-16-4
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| Cat. No. : | HY-123732 |
| M.Wt: | 322.42 |
| Formula: | C16H22N2O3S |
| Purity: | >98 % |
| Solubility: |
CRT0083914 (compound 12) is a subtype-selective non-carboxylate inhibitor of AKR1C3. CRT0083914 is applicable to the research of colon cancer[1].
In Vitro:CRT0083914 (0.1 nM to 100 μM) potently and selectively inhibits recombinant human AKR1C3 enzyme with an IC50 of 0.094 μM, while showing no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, or COX-2 at the tested concentrations[1].
CRT0083914 inhibits AKR1C3-dependent PR-104A metabolism in AKR1C3-overexpressing HCT-116 cells with an IC50 of 11 nM[1].
CRT0083914 binds to AKR1C3 with its 2-pyrrolidinone in the SP3 pocket and its sulfonamide-containing group in the SP1 pocket, making no direct contact with the enzyme's oxyanion hole residues[1].
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