AGK2

製品コード：S7577 純度：99.98%

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.

CAS No. 304896-28-4

サイズ	価格(税別)	在庫状況
5mg	JPY 18100	国内在庫あり
25mg	JPY 59600	国内在庫あり
100mg	JPY 167500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（30）

カスタマーフィードバック4个实验数据

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

AGK2関連製品

関連ターゲット	SIRT1 SIRT2 SIRT3 SIRT6 SIRT5	もっと見る
関連製品	Selisistat (EX 527) SRT1720 HCl Sirtinol Quercetin Nicotinamide Fisetin 3-TYP OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Nicotinamide Riboside Chloride Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 NRD167 Inauhzin CAY10602	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Angiogenesis Related compound Library TGF-beta/Smad compound library Cytoskeletal Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound Library	もっと見る

シグナル伝達経路

Sirtuinシグナル伝達経路

Sirtuin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HCT116	Function assay	10 uM	8 hrs	Inhibition of SIRT2 in human HCT116 cells assessed as increase in acetylated alpha-tubulin at 10 uM after 8 hrs by Western blot analysis	22642300
SH-SY5Y	Neuroprotective assay	1 to 10 uM	30 mins	Neuroprotective activity against oligomeric alpha-synuclein-induced cytotoxicity in human SH-SY5Y cells assessed as increase in cell growth at 1 to 10 uM preincubated for 30 mins followed by alpha-synuclein addition measured after 72 hrs by MTT assay	26982234
MCF7	Function assay	10 to 50 uM	24 hrs	Inhibition of SIRT2 in human MCF7 cells assessed as increase in alpha-tubulin K40 acetylation level at 10 to 50 uM after 24 hrs in presence of TSA by Western blot analysis	28135086
H4	Function assay		24 hrs	Inhibition of SIRT2 in H4 cells co-transfected with alphaSyn and synphilin1 assessed as enlarged alphaSyn inclusions after 24 hrs	17588900
30PT	Cytotoxicity assay		72 hrs	Cytotoxicity against human 30PT cells after 72 hrs by Cell-titer GLo assay, CC50=9.6μM	22931526
30P	Cytotoxicity assay		72 hrs	Cytotoxicity against human 30P cells after 72 hrs by Cell-titer GLo assay, CC50=12.5μM	22931526
30PT	Cytotoxicity assay		72 hrs	Cytotoxicity against human 30PT cells after 72 hrs by celltiter-glo luminescent assay, CC50=9.6μM	23189967
30P	Cytotoxicity assay		72 hrs	Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay, CC50=12.5μM	23189967
U373	Antiproliferative assay		72 hrs	Antiproliferative activity against human U373 cells after 72 hrs by MTT assay, IC50=47.6μM	28475330
Hs683	Cell cycle assay		24 to 48 hrs	Cell cycle arrest in human Hs683 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry	28475330
U373	Cell cycle assay		24 to 48 hrs	Cell cycle arrest in human U373 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry	28475330
Hs683	Cell cycle assay		24 to 48 hrs	Cell cycle arrest in human Hs683 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry	28475330
U373	Cell cycle assay		24 to 48 hrs	Cell cycle arrest in human U373 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry	28475330
rat embryo midbrain	Function assay			Protection of dopaminergic cell death in rat embryo midbrain transduced with lentivirus encoding alphaSyn-A53T mutant assessed as tyrosine hydroxylase positive cells	17588900
HeLa	Function assay			Inhibition of over-expressed SIRT2 immunoprecipitated from HeLa cells transfected with SIRT2-myc expression construct	17588900
Escherichia coli cells	Function assay			Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=5.5μM	22931526
Escherichia coli cells	Function assay			Inhibition of human recombinant SIRT1 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=38μM	22931526
Escherichia coli BL21 (DE3)	Function assay			Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=1.56μM	25275824
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生物活性

製品説明

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.

Targets

SIRT2 ^[1]
(Cell-free assay)

3.5 μM

In Vitro
In vitro	In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. ^[1] AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. ^[2] SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability. ^[3]

In Vivo
In Vivo	In drosophila model of parkinson's disease, AGK2 rescues α-Syn–mediated toxicity and modify aggregation. ^[1]
動物実験	動物モデル	Drosophila model of parkinson
	投与量	1mM
	投与経路	--

参考
[1] Outeiro TF, et al. Science.?007, 317(5837), 516-519. [2] He X, et al. Biochem Biophys Res Commun. 2012, 417(1), 468-472. [3] Petrilli A, et al. Oncotarget. 2013, 4(12), 2354-2365.

参考

化学情報

分子量	434.27	化学式	C₂₃H₁₃Cl₂N₃O₂
CAS No.	304896-28-4	SDF	Download AGK2 SDFをダウンロードする
Smiles	C1=CC2=C(C=CC=N2)C(=C1)NC(=O)C(=CC3=CC=C(O3)C4=C(C=CC(=C4)Cl)Cl)C#N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 4 mg/mL ( (9.21 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):