K00546

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K00546  纯度: 98.78%

K00546 是一种有效的 CDK1 和 CDK2 抑制剂，对 CDK1/cyclin B 和 CDK2/cyclin A 的 IC50 分别为 0.6 nM 和 0.5 nM。K00546 也是一种有效的 CDC2 样激酶 1 (CLK1) 和 CLK3 抑制剂，IC50 分别为 8.9 nM 和 29.2 nM。

K00546

K00546 Chemical Structure

CAS No. : 443798-47-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3080 In-stock
5 mg ￥2800 In-stock
10 mg ￥4500 In-stock
50 mg ￥13000 In-stock
100 mg ￥20000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively[1][2][3].

IC50 & Target

Cdk1/cyclin B

0.6 nM (IC50)

cdk2/cyclin A

0.5 nM (IC50)

CLK1

8.9 nM (IC50)

CLK3

29.2 nM (IC50)

GSK-3

140 nM (IC50)

VEGF-R2

32 nM (IC50)

体外研究
(In Vitro)

K00546 binds to the SLK ATP-binding site forming three hydrogen bonds with the kinase hinge residues E109 and C111. The sulphamoyl moiety of K00546 also interacts with the main chain of L40[1].
K00546 (compound 3n) also inhibits PKA, casein kinase-1, MAP kinase (ERK-2), calmodulin kinase, VEGF-R2, GSK-3 and PDGF-Rβ with IC50 values of 5.2 μM, 2.8 μM, 1.0 μM, 8.9 μM, 0.032 μM, 0.14 μM and 1.6 μM, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

425.44

Formula

C15H13F2N7O2S2
CAS 号

443798-47-8
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 : 100 mg/mL (235.05 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3505 mL 11.7525 mL 23.5051 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL
10 mM 0.2351 mL 1.1753 mL 2.3505 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。
参考文献

  • [1]. Ashley C W Pike, et al. Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites. EMBO J. 2008 Feb 20;27(4):704-14.

    [2]. Ronghui Lin, et al. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.

    [3]. Oleg Fedorov, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76.

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