MARK-IN-2

目录号: GC31280纯度: >98%

MARK-IN-2是一种有效的微管亲和力调节激酶(MARK)抑制剂，IC50为5nM。

Cas No.: 1314893-26-9

规格	价格	库存	数量	操作
250mg	询价	现货	1
500mg	询价	现货	1

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文献被引

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Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.

MARK-IN-2 (Compound 27) is a potent MARK inhibitor. Inhibition of MARK represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease. MARK-IN-2 inhibits MARK3 with an IC50 of 5 nM. MARK-IN-2 also inhibits MARK3 in primary cell culture of rat cortical neurons with an IC50 of 280 nM[1].

Characterization of the i.v. pharmacokinetic properties of MARK-IN-2 in rat and dog reveals reasonable volumes of distribution but moderate to high clearance and short half-lives. MARK-IN-2 (Compound 27) has moderate terminal elimination half-life (t1/2=0.7 h, and 1 h for rat and dog) [1].

[1]. Sloman DL, et al. Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4362-6.

实验参考方法 Experimental Reference Method

Cell experiment:

The cell biochemical potency of the below described MARK inhibitors (e.g., MARK-IN-2) is evaluated by measuring their ability to block the phosphorylation of Tau at S262 in primary cell culture of rat cortical neurons induced by the action of Okadaic acid[1].

Animal experiment:

Rats[1]Male Sprague-Dawley Rats are via a previously implanted venous catheter at 1 mL/kg and by gastric gavage at 5 mL/kg. Male Beagle Dogs are dosed via a saphenous vein indwelling catheter at 0.5 mL/kg and by gastric gavage at 5 mL/kg. Blood samples are collected into tubes containing EDTA at pre-dose and at 5 (intravenously administered drugs only), 15, and 30 min and 1, 2, 4, 6, 8, 12, and 24 h after drug administration. After sampling, whole blood is centrifuged at 14,000 rpm for 5 min, and plasma was stored frozen at -20ºC until the day of analysis[1].

References:

[1]. Sloman DL, et al. Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4362-6.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

1314893-26-9

SMILES

O=C(C1=CC(C2=C3N=CC(Cl)=CN3N=C2)=C(C)S1)N[C@H]4C(F)(F)CCC[C@H]4N

分子式

C₁₈H₁₈ClF₂N₅OS

分子量

425.88 g/mol

溶解性

DMSO : 25 mg/mL (58.70 mM; Need ultrasonic)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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