Name: Leucettinib-92
Brand: TargetMol
SKU: T79562
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

1 mg

¥ 593

8-10周

5 mg

待询

现货

生物活性

产品描述	Leucettinib-92 is a small-molecule inhibitor of the DYRK and CLK kinase families that exhibits differential inhibitory activity across multiple kinases, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3, supporting its use in kinase signaling and regulatory mechanism research.
靶点活性	CLK3:0.8 μM, DYRK1A:124 nM, CLK2:39 nM, DYRK1B:204 nM, DYRK2:0.16 μM, CLK4:5.2 nM, CLK1:147 nM, DYRK3:1.0 μM, GSK3:2.78 μM, DYRK4:0.52 μM
体外活性	Leucettinib-92（0.1-10 μM；3分钟）可与SH-SY5Y细胞内DYRK1A结合，并使其稳定至52°C以上的熔化温度。同时，Leucettinib-92（1 μM）有效抑制了两种DYRK1A底物（Thr212-Tau与Thr286-cyclin D1）的磷酸化作用[1]。
体内活性	方法：在糖尿病前期和糖尿病 GK 大鼠中体内给予 Leucettinib-92，评估 β 细胞增殖、胰岛素分泌、葡萄糖耐量和胰岛素敏感性。结果：Leucettinib-92 增加 β 细胞增殖和质量，预防高血糖发生，降低基础性高血糖，并改善葡萄糖耐量和胰岛素分泌[1]。
别名	Leucettinib-92, Leucettinib92, Leucettinib 92

化学信息

分子量	378.49
分子式	C₂₁H₂₂N₄OS
CAS No.	2732859-57-1
Smiles	N(C12CC3CC(C1)CC(C2)C3)C=4N/C(=C\C=5C=C6C(=CC5)N=CS6)/C(=O)N4
颜色	Yellow
物理性状	Solid

储存&溶解度

存储

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 20 mg/mL (52.84 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6421 mL	13.2104 mL	26.4208 mL	132.1039 mL
5 mM	0.5284 mL	2.6421 mL	5.2842 mL	26.4208 mL
10 mM	0.2642 mL	1.3210 mL	2.6421 mL	13.2104 mL
20 mM	0.1321 mL	0.6605 mL	1.3210 mL	6.6052 mL
50 mM	0.0528 mL	0.2642 mL	0.5284 mL	2.6421 mL