AGK2

目錄號(hào)：S7577 Purity: 99.98%

AGK2是一個(gè)有效的選擇性SIRT2抑制劑，IC50值為3.5 μM。對(duì)其他如SIRT1或SIRT3的抑制作用，在10倍以上的濃度時(shí)仍很微弱。

AGK2 Chemical Structure

CAS: 304896-28-4

規(guī)格	價(jià)格	庫存
5mg	797.57	現(xiàn)貨
25mg	2836.64	現(xiàn)貨
100mg	8155.18	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

AGK2相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	SIRT1 SIRT2 SIRT3 SIRT6 SIRT5	點(diǎn)擊展開
相關(guān)產(chǎn)品	Selisistat (EX 527) SRT1720 HCl Sirtinol Quercetin Fisetin 3-TYP OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 NRD167 Inauhzin CAY10602	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫血管生成相關(guān)化合物庫 TGF-beta/Smad信號(hào)通路庫細(xì)胞骨架信號(hào)通路化合物庫抗心血管疾病化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

AGK2是一個(gè)有效的選擇性SIRT2抑制劑，IC50值為3.5 μM。對(duì)其他如SIRT1或SIRT3的抑制作用，在10倍以上的濃度時(shí)仍很微弱。

靶點(diǎn)

SIRT2 ^[1]
(Cell-free assay)

3.5 μM

體外研究(In Vitro)
體外研究活性	在SIRT2-myc表達(dá)的HeLa細(xì)胞，AGK2有效抑制SIRT2的活性，并增加乙?；奈⒐艿鞍?。在初級(jí)中腦培養(yǎng)基中，AGK2保護(hù)多巴胺能神經(jīng)元免受α-Syn引起的毒性。^[1] AGK2誘導(dǎo)C6膠質(zhì)瘤細(xì)胞中細(xì)胞壞死和caspase-3依賴性細(xì)胞凋亡。^[2] SIRT2也能減少merlin突變型小鼠schwann細(xì)胞(MSCs)的生存能力，而基本不降低野生型MSC生存能力。^[3]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在帕金森氏病的果蠅模型中，AGK2清除α-Syn介導(dǎo)的毒性并修正聚合。^[1]
動(dòng)物實(shí)驗(yàn)	Animal Models	帕金森氏病的果蠅模型
	Dosages	1mM
	Administration	--

參考文獻(xiàn)
[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.

參考文獻(xiàn)

[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.

化學(xué)信息&溶解度

分子量	434.27	分子式	C₂₃H₁₃Cl₂N₃O₂
CAS號(hào)	304896-28-4	SDF	Download AGK2 SDF
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
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 10 mg/mL ( (23.02 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 10 mg/mL ( (23.02 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 4 mg/mL ( (9.21 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項(xiàng)

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):

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AGK2

產(chǎn)品質(zhì)控

AGK2相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持