GSK-3β inhibitor 3 - CAS:1448990-73-5

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GSK-3β inhibitor 3

目录号 : KM3690 CAS No. : 1448990-73-5 纯度 : 98%

Data Sheet 产品使用指南

GSK-3β inhibitor 3 是一种有效，选择性，不可逆和共价的糖原合酶激酶 3β (GSK-3β) 抑制剂，IC₅₀ 值为 6.6 μM。GSK-3β inhibitor 3 可用于急性早幼粒细胞白血病的研究。

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生物活性

GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC₅₀ of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.

体外研究

GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%.
GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells.
GSK-3β inhibitor 3 (12.5-100 μM; 24 h) significantly increases the percentage of apoptosis in a dose-dependent pattern in NB4 and NB4-R1 cells.

Cell Viability Assay

Cell Line:	NB4 and NB4-R1 cells
Concentration:	6.25, 12.5, 25, 50, 100 μM
Incubation Time:	24, 48 hours
Result:	Inhibited the cell viability, with IC₅₀s of 19.56 μM and 26.42 μM in NB4 and NB4-R1 cells at 24 h, respectively. Had little cytotoxicity on human normal liver cells (LO₂) and human umbilical vein endothelial cells (HUVECs).

Apoptosis Analysis

Cell Line:	NB4 and NB4-R1 cells
Concentration:	12.5, 25, 50, 100 μM
Incubation Time:	24 hours
Result:	Induced cell apoptosis.

体内研究

GSK-3β inhibitor 3 (compound 4-3) (15 mg/kg/d; i.p. for 2 weeks) inhibits tumor growth of mice by 75.97% relative to vehicle control.
GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T_1/2 of 14.2 h, high AUC values (AUC_last=3503.42 ng/mL•h), and maximum concentration (C_max=515 ng/mL) in mice.

Animal Model:	Balb/c female nude mice were injected leukemia cells
Dosage:	15 mg/kg/d
Administration:	I.p. for 2 weeks
Result:	Inhibited localized growth in NB4 cells. Had mild weight loss compared with control.

Animal Model:	Male ICR mice (30 g)
Dosage:	15 mg/kg (Pharmacokinetic Analysis)
Administration:	A single i.p.
Result:	T_1/2=14.2 h; AUC_last=3503.42 ng/mL•h; C_max=515 ng/mL.

分子式

C₁₈H₁₄FNO₂S

分子量

327.37

CAS号

1448990-73-5

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 : 250 mg/mL (763.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0546 mL	15.2732 mL	30.5465 mL
5 mM	0.6109 mL	3.0546 mL	6.1093 mL
10 mM	0.3055 mL	1.5273 mL	3.0546 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。