L-685458
Product Specifications
UNSPSC Description
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers[1][2].
Target Antigen
Apoptosis; γ-secretase
Type
Reference compound
Related Pathways
Apoptosis;Neuronal Signaling;Stem Cell/Wnt
Applications
Cancer-programmed cell death
Field of Research
Neurological Disease; Cancer
Assay Protocol
https://www.medchemexpress.com/L-685458.html
Purity
99.37
Solubility
DMSO : 83.3 mg/mL (ultrasonic;warming)
Smiles
O=C(N)[C@H](CC1=CC=CC=C1)NC([C@H](CC(C)C)NC([C@H](CC2=CC=CC=C2)C[C@@H](O)[C@@H](NC(OC(C)(C)C)=O)CC3=CC=CC=C3)=O)=O
Molecular Weight
672.85
References & Citations
[1]Shearman, M.S., Beher, D., Clarke, E.E., Lewis, H.D., Harrison, T., Hunt, P.,|[2]Guanghui Yang, et al. Structural basis of γ-secretase inhibition and modulation by small molecule drugs. Cell. 2021 Jan 21;184(2):521-533.e14.|[3]Jonas Sjölund, et al. Suppression of renal cell carcinoma growth by inhibition of Notch signaling in vitro and in vivo. J Clin Invest. 2008 Jan;118(1):217-28.|[4]Kazunori Kawaguchi, et al. Jagged1 DNA Copy Number Variation Is Associated with Poor Outcome in Liver Cancer. Am J Pathol. 2016 Aug;186(8):2055-2067.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-19369/L-685458-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-19369/L-685458-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
292632-98-5
Available Sizes
Curated Selection
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