價(jià)格 | ¥463 | ¥731 | ¥1492 |
包裝 | 5mg | 10mg | 50mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
中文名稱:化合物 Apoptosis Activator 2 | 英文名稱:MDK83190 |
CAS:79183-19-0 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 98.67% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T1772 |
名稱 | MDK83190 |
描述 | MDK83190 (Apoptosis Activator 2) is a potent apoptosis activator, induceing caspase-3 activation, PARP cleavage, and DNA fragmentation . |
細(xì)胞實(shí)驗(yàn) | All viable cells within the defined field of a microscope reticle grid are counted using a manual mechanical counter by an experimenter blinded to condition. Cells are scored viable on the basis of both positive staining with the vital dye calcein acetoxymethyl ester and the morphological criterion of a smooth, spherical soma. Counts of viable cells are made in four non-overlapping fields per culture well with each condition represented by 3 separate wells. The number of viable cells counts per well for vehicle-treated control conditions ranged from 100-200. All experiments are repeated in at least 3 independent culture preparations. Raw cell count data are statistically analyzed with one-way ANOVA, followed by between group comparisons using the Fisher LSD test (significance indicated by P < 0.05). Cell viability is presented graphically as a percentage of live cells in the vehicle-treated control condition.(Only for Reference) |
激酶實(shí)驗(yàn) | Cell-Free Apoptosis Assay: HeLa cell cytoplasmic extracts are prepared according to previously published reports. Apoptosis Activator 2 in DMSO are distributed into 96-well microtiter plates at a final concentration of 1 mM (final DMSO concentration is 1% vol/vol). To each well is added 250 μg of total protein from cytoplasmic extracts in HEB buffer (50 mM Hepes, pH 7.4/50 mM KCl/5 mM EGTA/2 mM MgCl), with 2 mM DTT, 2 μM cyto c, and 0.5 μM DEVD-AFC (Asp-Glu-Val-Asp-7-amino-4-trifluoromethylcoumarin) substrate in a total of 150 μL. Plates are incubated at 37 ℃, and fluorescence is read in a LJL Biosystems plate reader at 10-min intervals. |
體外活性 | Apoptosis Activator 2 (20 μM) 在降低的cyto c濃度下,將Apaf-1在細(xì)胞凋亡體中的比例增加1.5倍至33%。同時(shí),該化合物在降低的cyto c水平和caspase-3激活水平下,使caspase-3活化程度增加4倍。Apoptosis Activator 2強(qiáng)烈誘導(dǎo)caspase-3活化、PARP裂解和DNA片段化,最終以4 μM的IC50殺死細(xì)胞。Apoptosis Activator 2誘導(dǎo)PBL、HUVEC、Jurkat、Molt-4、CCRF-CEM、BT-549、MDA-MB-468和NCI-H23細(xì)胞凋亡,其IC50分別為50 μM、43 μM、4 μM、6 μM、9 μM、20 μM、44 μM和35 μM。在48個(gè)測(cè)試的腫瘤細(xì)胞系中,Apoptosis Activator 2對(duì)絕大多數(shù)腫瘤細(xì)胞系展現(xiàn)出細(xì)胞靜態(tài)效應(yīng),以10 μM的濃度在40個(gè)細(xì)胞系中抑制細(xì)胞生長(zhǎng)50-100%。[1] Apoptosis Activator 2通過(guò)觸發(fā)細(xì)胞凋亡體的形成引起細(xì)胞死亡。En1表達(dá)水平對(duì)Apoptosis Activator 2處理的腹側(cè)中腦培養(yǎng)存活率無(wú)顯著影響(-8.1 ± 6.0%)。如果使用其他三種試劑,存活率也沒有顯著變化(-10.7 ± 4.7%)。[2] Apoptosis Activator 2(10 μM)通過(guò)誘導(dǎo)凋亡DNA梯度和Tunel實(shí)驗(yàn)評(píng)估,在AGS細(xì)胞中誘導(dǎo)凋亡,并增強(qiáng)了抗TROP2偶聯(lián)脂質(zhì)體的凋亡誘導(dǎo)作用。[3] Cyclohexamide(10 μg/mL)或zVAD(50 μM)顯著保護(hù)神經(jīng)細(xì)胞培養(yǎng)物免受Apoptosis Activator 2的毒性。Apoptosis Activator 2(3 μM)導(dǎo)致大量神經(jīng)元出現(xiàn)細(xì)胞死亡涉及的凝集核。DHT(10 nM)或E2(10 nM)顯著保護(hù)神經(jīng)細(xì)胞培養(yǎng)物免受Apoptosis Activator 2的毒性。[4] |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 4.5 mg/mL (14.7 mM), Sonication is recommended. Ethanol : 1.5 mg/mL (5 mM) |
關(guān)鍵字 | Inhibitor | MDK83190 | Apoptosis | MDK-83190 | inhibit | MDK 83190 |
相關(guān)產(chǎn)品 | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
相關(guān)庫(kù) | 細(xì)胞焦亡化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌化合物庫(kù) | 已知活性化合物庫(kù) | 自噬庫(kù) | 細(xì)胞凋亡化合物庫(kù) | NO PAINS 化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 共價(jià)抑制劑庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.2651萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營(yíng)模式 | 貿(mào)易,試劑,定制,服務(wù) |
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