1. Metabolic Enzyme/Protease
  2. Aldose Reductase
  3. CRT0093964

CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC50=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer.

For research use only. We do not sell to patients.

CRT0093964

CRT0093964 Chemical Structure

CAS No. : 700856-05-9

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Description

CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC50=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer[1].

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.018 μM
Compound: 24
Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs
Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs
[PMID: 24411201]
In Vitro

CRT0093964 (0.1 nM-100 μM; 1 h) potently and selectively inhibits purified recombinant AKR1C3 with an IC50 of 0.11 μM; in contrast, this compound shows no inhibitory effect on AKR1C1, AKR1C2 or AKR1C4 at concentrations up to 30 μM[1].
CRT0093964 (1 nM-3 μM; 2 h pre-treatment) inhibits AKR1C3-dependent metabolism of PR-104A (HY-16405) in AKR1C3-overexpressing HCT-116 cells, with an IC50 of 0.018 μM, and exhibits higher potency in cellular assays than in purified enzyme assays[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

309.79

Formula

C15H20ClN3O2

CAS No.
SMILES

O=C(N1CCOCC1)N2CCN(C3=CC=C(Cl)C=C3)CC2

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Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CRT0093964
Cat. No.:
HY-124432
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