1. Cell Cycle/DNA Damage
  2. CDK
  3. BLINK15

BLINK15 是一种可渗透血脑屏障的 Cdk5 抑制剂。BLINK15 可降低 CDK5/p35 (IC50 = 29.34 nM) 和 CDK5/p25 (IC50 = 12.08 nM) 复合物的 CDK5 活性。BLINK15 具有抗糖尿病和神经保护作用。BLINK15 可降低 2 型糖尿病 (T2D) 小鼠的血糖,增强认知能力,并减少神经退行性病变。

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BLINK15 Chemical Structure

BLINK15 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice[1].

IC50 & Target

CDK9/Cyclin T

74.63 nM (IC50)

CDK1/Cly Y

35.84 nM (IC50)

CDK2/ClyA2

44.12 nM (IC50)

CDK5/p35

29.34 nM (IC50)

Cdk5/p25

12.08 nM (IC50)

体外研究
(In Vitro)

BLINK15 (50 nM-100 nM,24 小时) 可降低 CDK5/p35 (IC50 = 29.34 nM) 和 CDK5/p25 (IC50 = 12.08 nM) 复合物的 CDK5 活性[1]
BLINK15 (50 nM-100 nM,24 小时) 过表达 CDK5/p35 和 CDK5/p25 后的 N2A 细胞系中的 CDK5 活性下降[1]
BLINK15 (25-500 μM,24 小时) 在所有剂量下均可在 HEK293T、HepG2 和 N2A 细胞系中维持 50% 以上的细胞活力[1]
BLINK15 (100-500 μM,7 小时) 显示出穿越血脑屏障 (BBB) 并进入中枢神经系统的能力[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BLINK15 (20-40 mg/kg/天,i.p.,20 天) 显示可缓解 HFD 喂养小鼠模型中的 2 型糖尿病相关症状[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: High-fat diet (HFD)-fed (3-4 weeks), four-week-old male C57BL/6J mice (n=40)[1]
Dosage: 20 mg/kg/day, 40 mg/kg/day
Administration: Intraperitoneal injection (i.p.), 20 days, 3 months after HFD-fed for 3-4 weeks
Result: Demonstrated rescued symptoms caused by T2D including gaining of body weight, glucose tolerance test (GTT) and insulin tolerance test (ITT) level.
Alleviated cognitive impairment including rescued muscle strength and prevent anxiety, showing mitigated adverse effects of HFD level.
Rescued memory and spatial learning impairments in T2D mouse models with 40 mg/kg/day dosage but no effect with 20 mg/kg/day.
Significantly reduced CDK5 activity even in the presence of p25.
分子量

511.32

Formula

C24H19BrN2O6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BLINK15
目录号:
HY-173348
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