L-685,458

製品コードS7673 バッチS767301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₉H₅₂N₄O₆

分子量

672.85

CAS No.

292632-98-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (148.62 mM)

Ethanol (warmed with 50ºC water bath)

6 mg/mL (8.91 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with K_i of 17 nM.
in vitro	L-685,458 inhibits Aβ(40) formation in both Neuro2A and CHO cell lines overexpressing human AβPP695, and in SHSY5Y cells overexpressing the construct spβA4CTF with IC50 of 402 nM, 113 nM, and 48 nM, respectively, with the potency for reduction of Aβ(42) being about 2-fold lower. ^[1] In Tca8113 cells, L-685,458 inhibits cell growth by inducing G0–G1 cell cycle arrest and apoptosis. ^[2] In a T-cell acute lymphoblastic leukemia cell line, pre-treatment with L-685,458 enhances the anti-proliferative effect of imatinib. ^[3] L685,458 also significantly reduces HSV-1 replication in tissue culture by inhibiting signal peptide peptidase (SPP). ^[4]

製品説明

L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with K_i of 17 nM.

in vitro

L-685,458 inhibits Aβ(40) formation in both Neuro2A and CHO cell lines overexpressing human AβPP695, and in SHSY5Y cells overexpressing the construct spβA4CTF with IC50 of 402 nM, 113 nM, and 48 nM, respectively, with the potency for reduction of Aβ(42) being about 2-fold lower. ^[1] In Tca8113 cells, L-685,458 inhibits cell growth by inducing G0–G1 cell cycle arrest and apoptosis. ^[2] In a T-cell acute lymphoblastic leukemia cell line, pre-treatment with L-685,458 enhances the anti-proliferative effect of imatinib. ^[3] L685,458 also significantly reduces HSV-1 replication in tissue culture by inhibiting signal peptide peptidase (SPP). ^[4]

プロトコル(参考用のみ)

キナーゼアッセイ	HTRF Immunoassay for Aβ Quantitation
キナーゼアッセイ	Homogeneous time-resolved fluorescence (HTRF) immunoassay methodology uses fluorescence resonance energy transfer (FRET) between two fluorophores, a donor EuK and a modified allophycocyanine pigment acceptor molecule, XL-665. When in proximity, nonradiative FRET takes place from nitrogen laser-excited EuK to XL-665, resulting in the emission of an amplified long-lived fluorescence signal. Briefly, in a typical 96-well plate assay, each well contains 0.75 nM antibody-EuK, 1.0 nM antibody-biotin, 2.0 nM SA-XL665, and 0.1−0.2 M potassium fluoride. Samples of conditioned cell culture medium or synthetic peptide standards and culture medium alone are added to give a total assay volume of 200 μL/well. Blank values are determined by the inclusion of 1.0 nM nonbiotinylated antibody in place of the biotinylated antibody. Following mixing, the reaction mixture is left at 4 °C to reach equilibrium binding, and then read on the Discovery HTRF microplate analyzer using the manufacturer
細胞アッセイ	細胞株	Tca8113 cells
	濃度	~5.0 μM
	反応時間	48 h
	実験の流れ	The in vitro growth rate of Tca8113 cells treated with L-685,458, is measured by MTT. Briefly, Tca8113 cells are seeded in 96-well plates. On the day of harvest, 100 μL of spent medium is replaced with an equal volume of fresh medium containing 10% MTT 5 mg ml−1 stock. Plates are incubated at 37°C for 4 h, then 100 μl of DMSO is added to each well, and then plates are shaken at room temperature for 10 min. The absorbance is measured at 570 nm.

参考

[4] Allen SJ, et al. Exp Eye Res. 2014 Jun;123:8-15.

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カスタマーフィードバック

: Data from [Data independently produced by , , Sci Rep, 2017 , 7(1):4983]

: Data from [Data independently produced by , , PLoS One, 2017, 12(3):e0173240]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182]	PubMed: 36248745
Carboxy-terminal fragment of amyloid precursor protein mediates lipid droplet accumulation upon γ-secretase inhibition [ Biochem Biophys Res Commun, 2021, 570:137-142]	PubMed: 34280617
A novel rhamnoside derivative PL402 up-regulates matrix metalloproteinase 3/9 to promote Aβ degradation and alleviates Alzheimer's-like pathology. [ Aging (Albany NY), 2020, 12(1):481-501]	PubMed: 31901901
A cellular complex of BACE1 and γ-secretase sequentially generates Aβ from its full-length precursor. [ J Cell Biol, 2019, 218(2):644-663]	PubMed: 30626721

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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