AZ191

製品コードS7338 バッチS733801

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	C₂₄H₂₇N₇O
	分子量	429.52	CAS No.	1594092-37-1
Solubility (25°C)*	体外	DMSO	86 mg/mL (200.22 mM)
		Ethanol	1 mg/mL (2.32 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	AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
in vitro	AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21^Cip1 and p27^Kip1, and increases cell-cycle progression. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro DYRK kinase assay
キナーゼアッセイ	EGFP–DYRK1A, EGFP–DYRK1B or EGFP–DYRK2 was immunoprecipitated from whole-cell lysate and pre-incubated in the absence or presence of various concentrations of AZ191 or harmine for 5 min at room temperature (20°C) and then assayed for kinase activity by incubating with 50 μM Woodtide, with two additional lysine residues attached to the N-terminus to allow it to bind to P81 paper (KKSSCYVDRKIYTYIQSRFY), 50 mM Tris/HCl (pH 7.5), 0.1 mM EGTA, 0.1% 2-mercaptoethanol, 10 mM MgCl2 and 0.1 mM [γ-³²P]ATP in a total volume of 50 μl for 25 min at 30°C.

参考

[1] Ashford AL, et al. Biochem J. 2014, 457(1), 43-56.

カスタマーフィードバック

: , , Cell Death Dis, 2014, 5:e1548.

: Data from [Data independently produced by , , Sci Rep, 2016, 6:37052.]

: Data from [Data independently produced by , , Oncotarget, 2017, 8(1):833-845]

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 DYRK1B-dependent pathway suppresses rDNA transcription in response to DNA damage [ Nucleic Acids Res, 2021, gkaa1290]	PubMed: 33469661
TROAP switches DYRK1 activity to drive hepatocellular carcinoma progression [ Cell Death Dis, 2021, 12(1):125]	PubMed: 33500384
TROAP switches DYRK1 activity to drive hepatocellular carcinoma progression [ Cell Death Dis, 2021, 12(1):125]	PubMed: 33500384
Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors. [ JCI Insight, 2020, 5(1)]	PubMed: 31821176
Serum deprivation initiates adaptation and survival to oxidative stress in prostate cancer cells [ Sci Rep, 2020, 10(1):12505]	PubMed: 32719369
Targeting DYRK1B suppresses the proliferation and migration of liposarcoma cells [ Oncotarget, 2018, 9(17):13154-13166]	PubMed: 29568347
Inhibitors of dual-specificity tyrosine phosphorylation-regulated kinases (DYRK) exert a strong anti-herpesviral activity. [Hutterer C, et al. Antiviral Res, 2017, 143:113-121]	PubMed: 28400201
DYRK1B blocks canonical and promotes non-canonical Hedgehog signaling through activation of the mTOR/AKT pathway. [Singh R, et al. Oncotarget, 2017, 8(1):833-845]	PubMed: 27903983
Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells [Li Z, et al. Cancer Lett, 2016, 370(2):332-44]	PubMed: 26586345
Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. [Yan Y, et al. Sci Rep, 2016, 6:37052]	PubMed: 27845389

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。