FM-381

製品コードS8541 バッチS854101

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₄N₆O₂
	分子量	428.49	CAS No.	2226521-65-7
Solubility (25°C)*	体外	DMSO	20 mg/mL (46.67 mM)
		Ethanol	2 mg/mL (4.66 mM)
		Water	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	FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.
in vitro	FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 µM^[1].

製品説明

FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.

in vitro

FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 µM^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CD4+ T Cell
	濃度	0, 10, 50, 100, 300 nM
	反応時間	1 h
	実験の流れ	T cells were purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells were incubated for 1 hr with JAK inhibitors or DMSO control and stimulated with cytokines for 30 min. The cells were lysed, and the proteins were separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest were blotted with specific antibodies and visualized with an infrared imaging system.

参考

[1] Forster M, et al. Cell Chem Biol. 2016, 23(11):1335-1340.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation. [ Commun Biol, 2020, 3:8]	PubMed: 31909200

A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation. [ Commun Biol, 2020, 3:8]

PubMed: 31909200

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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