L-685458

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L-685458

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

292632-98-5

L-685,458

L-685458 是一种有效的过渡状态模拟(TSA) γ-分泌酶 (γ-secretase) 抑制剂 (GSI)。L-685458 抑制淀粉样 β-蛋白前体 γ-分泌酶活性，IC₅₀为 17 nM，选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。L-685458 抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解，IC₅₀分别为 301.3 nM 和 351.3 nM。L-685458 可用于阿尔茨海默病 (AD) 和癌症的研究。

生物活性

L-685458 is a potent transition state analog (TSA)γ-secretaseinhibitor (GSI). L-685458 inhibits amyloid β-protein precursorγ-secretaseactivity withIC₅₀of 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].

体外研究
(In Vitro)

L-685458 reduces both Aβ(40) and Aβ(42) peptide formation in 3 different cells. It against Neuro2A h AβPP695, CHO h AβPP695, and SHSY5 spβA4CTF reduction of Aβ(40) with IC₅₀values of 402 nM, 113 nM and 48 nM, respectively. And the IC₅₀values are 775 nM, 248 nM, 67 nM, respectively^[1].
L-685458 (5-40 μM; 24 hours) leads to a dramatic downregulation of Hes-1 in 786-O cells^[3].
L-685458 has inhibitory effects in hepatoma cell lines, it against Huh7, HepG2, HLE and SKHep1 cells with IC₅₀of 12.91 μM, 12.69 μM, 21.76 μM and 12.18 μM, respectively^[4].

体内研究
(In Vivo)

L-685458 (percutaneous administration; 5 mg/kg; 2 weeks) has antitumor effects in mouse hepatoma models. L-685458 inhibits EpCAM production except in necrotic areas. And HES1 staining is also diminished in the nucleus^[4].

Animal Model:	NOD-SCID Mouse Hepatoma Model^[4]
Dosage:	5 mg/kg
Administration:	Percutaneous administration; 5 mg/kg; 2 weeks
Result:	Exhibited anti-tumor activities in vivo.

分子量

672.85

性状

Solid

Formula

C₃₉H₅₂N₄O₆

CAS 号

292632-98-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 83.3 mg/mL(123.80 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.4862 mL	7.4311 mL	14.8622 mL
5 mM	0.2972 mL	1.4862 mL	2.9724 mL
10 mM	0.1486 mL	0.7431 mL	1.4862 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。