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

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.

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LKY-047 Chemical Structure

LKY-047 Chemical Structure

CAS No. : 1954681-29-8

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25 mg USD 720 In-stock
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Based on 1 publication(s) in Google Scholar

LKY-047 Related Antibodies

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View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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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].

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

LKY-047 Related Antibodies
Molecular Weight

421.40

Formula

C23H19NO7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O[C@H]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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (39.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3730 mL 11.8652 mL 23.7304 mL
5 mM 0.4746 mL 2.3730 mL 4.7461 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3730 mL 11.8652 mL 23.7304 mL 59.3261 mL
5 mM 0.4746 mL 2.3730 mL 4.7461 mL 11.8652 mL
10 mM 0.2373 mL 1.1865 mL 2.3730 mL 5.9326 mL
15 mM 0.1582 mL 0.7910 mL 1.5820 mL 3.9551 mL
20 mM 0.1187 mL 0.5933 mL 1.1865 mL 2.9663 mL
25 mM 0.0949 mL 0.4746 mL 0.9492 mL 2.3730 mL
30 mM 0.0791 mL 0.3955 mL 0.7910 mL 1.9775 mL
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LKY-047 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

LKY-0471954681-29-8LKY047LKY 047Cytochrome P450CYPsCYP2J2DecursinO-demethylaseterfenadinehydroxylaseebastineInhibitorinhibitorinhibit

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