1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. LKY-047

LKY-047 

Cat. No.: HY-117026
Handling Instructions

LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.

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

LKY-047 Chemical Structure

LKY-047 Chemical Structure

CAS No. : 1954681-29-8

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Description

LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A[1].

IC50 & Target[1]

CYP2J2

1.7 μM (IC50)

In Vitro

LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 μM and 2.61 μM, respectively. LKY-047 also acted as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a Ki value of 3.61 μM[1].
At 20 μM LKY-047 concentration, approximately 20-fold greater than the Ki value, LKY-047 is found to inhibit CYP2J2 by 85.3%, and only slightly affecting the enzyme activities of the other P450s tested. LKY-047 weakly inhibits CYP2D6 enzyme activity (37.2%) at 20 μM concentration[1].

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

Molecular Weight

421.40

Formula

C₂₃H₁₉NO₇

CAS No.

1954681-29-8

SMILES

O=C(O[[email protected]]1CC(C=C(C=CC(O2)=O)C2=C3)=C3OC1(C)C)/C=C/C4=CC=C([N+]([O-])=O)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

LKY-047LKY047LKY 047Cytochrome P450CYPsCYP2J2DecursinO-demethylaseterfenadinehydroxylaseebastineInhibitorinhibitorinhibit

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LKY-047
Cat. No.:
HY-117026
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