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product-image-AAA228005_STRUCTURE13.gif Structure (Benzyl-PEG7-THP, CAS 230620-75-4)

LKY-047 biochemical

LKY-047

Purity
98%
Synonyms
LKY-047; N/A; LKY-047 biochemical
Ordering
Purity/Purification
98%
CAS
1954681-29-8
Targets&IC50
CYP2J2:1.7 uM (IC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with K i values of 0.96 uM and 2.61 uM, respectively. LKY-047 also acted as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a K i value of 3.61 uM[1]. At 20 uM 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 uM concentration[1].
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years

Structure

(Benzyl-PEG7-THP, CAS 230620-75-4)

product-image-AAA228005_STRUCTURE13.gif Structure (Benzyl-PEG7-THP, CAS 230620-75-4)

Structure

(Benzyl-PEG7-THP, CAS 230620-75-4)

product-image-AAA228005_STRUCTURE15.gif Structure (Benzyl-PEG7-THP, CAS 230620-75-4)
Related Product Information for LKY-047 biochemical
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC 50 of 1.7 uM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
References
1. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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Product Notes

The LKY-047 (Catalog #AAA228005) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "LKY-047, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

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