IC261

製品コードS8237 バッチS823701

化学情報

	Synonyms	SU-5607	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₁₇NO₄
	分子量	311.33	CAS No.	186611-52-9
Solubility (25°C)*	体外	DMSO	62 mg/mL (199.14 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.
in vitro	IC261 leads to a p53-dependent arrest of the cells with a DNA content of 4 N. It can produce effects on cell cycle progression that are indistinguishable from an established spindle poison and are dependent on the p53 status of the cells^[1].
in vivo	Intrathecal injection of a CK1 inhibitor IC261 attenuates neuropathic pain behaviors. CK1 inhibitors are found to be effective in reducing spinal excitatory response elicited by the presynaptic electrical stimulation only in neuropathic mice^[2]. Targeting CK1 isoforms by IC261 influences both pancreatic tumour cell growth and apoptosis sensitivity in vitro and the growth of induced tumours in vivo^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MEFs
	濃度	1 μM
	反応時間	12 h, 24 h, 48 h
	実験の流れ	Cultures of MEFs of dierent genotypes (p53^+/+, p53^+/-, p53^-/-) are treated with the inhibitor IC261 in the low micromolar range (1 μM). After 12, 24, 48 hours exposure, the effects of IC261 on cell cycle distribution are measured by flow cytometry.
動物実験	動物モデル	Male C57BL/6J mice
	投薬量	0.1-1 nmol
	投与方法	intrathecal administration

参考

[4] Liu F, et al. Proc Natl Acad Sci U S A. 2001, 98(20):11062-11068.

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PP5 (PPP5C) is a phosphatase of Dvl2 [ Sci Rep, 2018, 8(1):2715]	PubMed: 29426949

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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