KY-05009 - CAS:1228280-29-2

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KY-05009

目录号 : KM3029 CAS No. : 1228280-29-2 纯度 : 98%

Data Sheet 产品使用指南

KY-05009 是一种具有 ATP 竞争性的 TNIK 抑制剂，K_i 为 100 nM。KY-05009 在药理上抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制 TNIK 的蛋白表达和 Wnt 靶基因的转录活性，并诱导癌细胞凋亡。KY-05009 具有抗癌活性。

规格	价格	是否有货
5mg		In-stock
25mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a K_i of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.

体外研究

KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner.
KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner.
KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.
. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment inhibits the IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4.

Cell Proliferation Assay

Cell Line:	RPMI8226 cells
Concentration:	0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time:	24 hours
Result:	Inhibited the proliferation of RPMI8226 cells.

Apoptosis Analysis

Cell Line:	RPMI8226 cells
Concentration:	1 μM, 3 μM, 10 μM
Incubation Time:	48 hours, 72 hours
Result:	Induced the binding of fluorescent Annexin V and 7-amino-actinomycin D (7-AAD) uptake.

RT-PCR

Cell Line:	RPMI8226 cells
Concentration:	3 μM
Incubation Time:	1 hour
Result:	Suppressed the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.

Western Blot Analysis

Cell Line:	RPMI8226 cells
Concentration:	3 μM
Incubation Time:	9 hours
Result:	The IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4 were inhibited.

分子式

C₁₈H₁₆N₄O₂S

分子量

352.41

CAS号

1228280-29-2

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 : 83.33 mg/mL (236.46 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8376 mL	14.1880 mL	28.3760 mL
5 mM	0.5675 mL	2.8376 mL	5.6752 mL
10 mM	0.2838 mL	1.4188 mL	2.8376 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.90 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。