UK 383367

製品コードS2224 バッチS222452

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	C₁₅H₂₄N₄O₄
	分子量	324.38	CAS No.	348622-88-8
Solubility (25°C)*	体外	DMSO	65 mg/mL (200.38 mM)
		Ethanol	16 mg/mL (49.32 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	UK-383367 is a procollagen C-proteinase (BMP-1) inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.
in vitro	UK-383367 is effective at penetrating human skin. ^[1] UK-383367 inhibits collagen deposition with IC50 of ~2 μM. UK-383367 has modest affinity for all the PDE-4 subtypes PDE-4a, PDE-4b, PDE-4c and PDE-4d with IC50 of 1.8 μM, 1.5 μM, 2.4 μM and 0.9 μM, respectively. ^[2] UK-383367 is a weakly acidic compound and lipophilic. ^[3]
in vivo	Plasma protein binding values for UK-383367 in rat, dog and human are 95%, 93% and 94%, respectively. UK-383367 following incubation in rat plasma results in the half-life of 49 min. UK-383367 following single intravenous administration (2 mg/kg) to rat results in the plasma clearance of 157 mL min⁻¹ kg⁻¹, the volume of distribution of 12 L kg⁻¹, and an elimination half-life of 0.8 hour. UK-383367 following single intravenous administration (0.5 mg/kg) to dog results in the plasma clearance of 35 mL min⁻¹ kg⁻¹, the volume of distribution of 4.6 L kg⁻¹, and an elimination half-life of 1.5 hours. UK-383367 following oral administration (2 mg/kg) to dog results in C_max of 110 ng/mL, T_max of 0.5-1.5 hour and oral bioavilability of 13%. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	PCP Inhibition
キナーゼアッセイ	Human PCP is purified from supernatant of stable transfected CHO cells using hydrophobic interaction column followed by Superdex 200 gel filtration. Total protein (4 μg) of this enzyme preparation is incubated with various concentrations of UK-383367 and 3 μM substrate in assay buffer (50 mM Tris-Base, pH 7.6 containing 150 mM NaCl, 5 mM CaCl₂, 1 μM ZnCl₂, and 0.01% Brij 35). The assay is performed in 96-well black fluorimeter plates and fluorescence is read continuously in a fluorimeter over 2.5 h (λ_ex = 340 nm, λ_em = 485 nm) at a constant 37 ℃ with shaking. Release of the fluorogenic signal is in linear correlation to PCP activity. Reading of the mean velocity from 30 min after start of experiment until 2.5 hours is calculated by the Biolise software. IC50 values are calculated by plotting % inhibition values against compound concentration using Tessela add-in for Excel spreadsheet.
動物実験	動物モデル	Sprague–Dawley rats
	投薬量	2 mg/kg
	投与方法	Intravenously

参考

カスタマーフィードバック

: Data from [Data independently produced by , , BMC Cancer, 2018, 18:508 ]

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：

Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer [ ACS Chem Biol, 2021, 10.1021/acschembio.0c01000]	PubMed: 33765766
Poldip2 mediates blood-brain barrier disruption and cerebral edema by inducing AQP4 polarity loss in mouse bacterial meningitis model [ CNS Neurosci Ther, 2020, 10.1111/cns.13446]	PubMed: 32790044
Extracellular BMP1 is the major proteinase for C-terminal proteolysis of type I procollagen in lung fibroblasts [ Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00012.2020]	PubMed: 33206546
[ Am J Physiol Renal Physiol, 2019, ]	PubMed: 31545926
Clinical significance and biological role of cancer-derived Type I collagen in lung and esophageal cancers [ Thorac Cancer, 2019, 10(2):277-288]	PubMed: 30604926
Upregulation of bone morphogenetic protein 1 is associated with poor prognosis of late-stage gastric Cancer patients [Hsieh YY, et al. BMC Cancer, 2018, 18(1):508]	PubMed: 29720137

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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