NCT-501

製品コードS7941 バッチS794101

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	C₂₁H₃₂N₆O₃
	分子量	416.52	CAS No.	1802088-50-1
Solubility (25°C)*	体外	DMSO	32 mg/mL warmed with 50ºC water bath (76.82 mM)
		Ethanol	25 mg/mL (60.02 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	NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
in vitro	In Caco-2 cell line, NCT-501 exhibits excellent permeability. ^[1]
in vivo	In CD1 Mice, NCT-501 is well absorbed and distributed but rapidly metabolized and/or excreted. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	General Protocol for ALDH Enzymatic Assays
キナーゼアッセイ	Briefly, an amount of 3 μL of enzyme (final concentration 20, 50, 20, and 5 nM for ALDH1A1, ALDH1B1, ALDH2, and ALDH3A1, respectively) or assay buffer (100 mM HEPES, pH 7.5, with 0.01% Tween 20) is dispensed into a 1536-well solid-bottom black plate followed by pin-tool transfer (23 nL) of candidate inhibitors (final concentration range 968 pM to 57.2 μM) and control (Bay 11-7085, final concentration range from 1.31 nM to 2.86 μM). Samples are incubated (rt, protected from light) for 15 min followed by a 1 μL substrate addition of NAD+ and propionaldehyde (final concentrations of 1 mM and 80 μM, respectively, for ALDH1A1, ALDH1B1, and ALDH2; or NAD+ and benzaldehyde at 1 mM and 200 μM, respectively, for ALDH3A1). Plates are centrifuged at 1000 rpm for 15 s, then read in kinetic mode on a ViewLux high-throughput CCD imager equipped with standard UV fluorescence optics (340 nm excitation, 450 nm emission) for 10 min (ALDH1A1, ALDH1B1, ALDH2) or 4 min (ALDH3A1). The change in fluorescence intensity over the 4 or 10 min reaction period is normalized against no-inhibitor and no-enzyme controls, and the resulting percent inhibition data are fitted for biological activity. Disulfiram is used as internal standard with comparable activity to reported potency.

参考

[1] Yang SM, et al. J Med Chem. 2015, 58(15), 5967-5978.

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：

Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632]	PubMed: 37828768

Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632]

PubMed: 37828768

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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