1、ScriptaidCat. No.: HY-15489CAS No.: 287383-59-9分式: CHNO分量: 326.35作靶点: HDAC; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (459.63 mM)* “ means soluble, but saturation unknown.ConcentrationSo
2、lvent Mass 1 mg 5 mg 10 mg1 mM 3.0642 mL 15.3210 mL 30.6419 mL5 mM 0.6128 mL 3.0642 mL 6.1284 mL制备储备液10 mM 0.3064 mL 1.5321 mL 3.0642 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液BIOLOGICAL ACTIVITY物活性 Scriptaid 是种组蛋去酰化酶 ( HDAC) 抑制剂，可于癌症研究 。IC when it is combined with AZA, they enhance ER expression and induce a f
3、unctional ER protein1. Scriptaid and SAHA preferentially inhibit the Class I histone deacetylases, hdac1, 2, and 3. Scriptaid is a potent anti-T. gondii compound with low cytotoxicity, and the IC50 is 39 nM. Scriptaid has atypical effects in T. gondiiinfected HS68 cells2. Scriptaid inhibits the grow
4、th of HeLa cells with IC50 of 2 M at 48 h in a dose-dependent manner. Scriptaid also affects cell-cycle and apoptosis3.Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1体内研究 Scriptaid (3.5 g/g mouse, i.p.) clearly inhibits tumor growth in a xenograft mouse model1.PROTOCOLCell Assa
5、y 1 IC50 concentrations of Scriptaid are determined in MDA-MB-231, MDA-MB-435 and Hs578t cells by MTT assay. For cell growth assays, MDA-MB-231, MDA-MB-435, and Hs578t cells are plated at a cell density of 5000 cells/well in 12 well plates and treated with 1.0 g/mL Scriptaid for up to 3 days. Cells
6、are counted daily using a Coulter counter. Percent growth inhibition is determined by comparison of treated and untreated cells1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration 1Four to six week old athymic female nude mice are hou
7、sed under laminar flow hoods in an environmentally controlled pathogen free animal facility for the duration of experiments. Mice are injected with 2106 MDA-MB-231 human breast cancer cells into each flank. Tumors are allowed to grow to approximately 0.1 cm3 in diameter before treatment. Mice are th
8、en treated with Scriptaid (3.5 g/g mouse), TSA (0.5 g/g mouse), or DMSO vehicle intraperitoneally for five consecutive days with 2 days rest each week for a total of 4 weeks. Individual tumor measurements are recorded from each flank weekly1.MCE has not independently confirmed the accuracy of these
9、methods. They are for reference only.客户使本产品发表的科研献See more customer validations on www.MedChemEREFERENCES1. Keen JC, et al. A novel histone deacetylase inhibitor, scriptaid, enhances expression of functional estrogen receptor alpha (ER) in ER negative human breast cancer cells in combination with 5-a
10、za 2-deoxycytidine. Breast Cancer Res Treat. 2003 Oct;81(3):177-86.2. Strobl JS, et al. Scriptaid and suberoylanilide hydroxamic acid are histone deacetylase inhibitors with potent anti-Toxoplasma gondii activity in vitro. J Parasitol. 2007 Jun;93(3):694-700.3. Janaki Ramaiah M, et al. Scriptaid cau
11、se histone deacetylase inhibition and cell cycle arrest in HeLa cancer cells: A study on structural and functional aspects. Gene. 2017 Sep 5;627:379-386.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.Tel: 400-820-3792; 021-58955995 Fax: 021-
12、53700325 E-mail: techMedChemEMaster of Small Molecules 您边的抑制剂师 Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966.www.MedChemE2勌勌 Fax: 021-53700325 E-mail: techMedChemEMaster of Small Molecules 您边的抑制剂师www.MedChemE3 自 然 环 境 ， 并 限 制城 市 扩 张 的 规 模 。 各 城 市 应 重 点 为 所 有 市 民 提 供 便 捷 、 舒 适 和 高 效 的 公 共 交
13、通 服 务 、 较 为 经 济 的 住 房 、 公 用 设 施 和 其 他 公 共 服 务 。 此 外 ， 该 规 划 也 指 出 ， 产 业 发 展 依 然 是 未 来 城 市 发 展 的 重 要 组 成 部 分 ， 能 够 推 动 经 济 增 长 并 创 造 就 业 机 会 。 行 动 倡 议 提 出 的 “ 交 通 规 划 SL327Cat. No.: HY-15437CAS No.: 305350-87-2分式: CHFNS分量: 335.35作靶点: MEK作通路: MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solven
14、t -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 68 mg/mL (202.77 mM; Need ultrasonic)Ethanol : 0.1 mg/mL (0.30 mM; Need ultrasonic and warming)ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.9820 mL 14.9098 mL 29.8196 mL5 mM 0.5964 mL 2.9820 mL 5.9639 mL制备储备液10 mM 0.2982 mL 1.4910 mL 2.9820 mL请根据产品在不同溶剂
15、中的溶解度，选择合适的溶剂配制储备液体内实验 SL327 is prepared in vehicle (saline)6.1. BIOLOGICAL ACTIVITY物活性 SL327 抑制 MEK1 和 MEK2， IC50 分别为 180 nM 和 220 nM。IC they take significantly longer to find a hidden platform compared with vehicle-treated controls and also fail to use a selective search strategy during subsequent
16、 probe trials in which the platform is removed. Mice are injected with various concentrations of SL327 (10, 30, 50 mg/kg i.p.), and 1 hr later their hippocampi are removed and assayed for activated MAPK. SL327 attenuates phosphorylated MAPK levels in a dose-dependent manner. Administration of 10, 30
17、, or 50 mg/kg SL327 significantly attenuates p42 phospho-MAPK levels (F=20.90, P0.0001;10 mg/kg SL327 vs. vehicle, P0.05, and 30 and 50 mg/kg SL327 vs. vehicle, P0.001). Injection with 30 or 50 mg/kg SL327 also significantly reduces p44 phospho-MAPK levels (F=5.627, P0.005;30 mg/kg vs. vehicle, P0.0
18、5, and 50 mg/kg SL327 vs. vehicle, P0.01)2.PROTOCOLKinase Assay 2 Protein kinase assays are performed. All kinase assays are started by adding enzyme to a mixture that included -32PATP and substrate. This mixture is then incubated at 30C or 37C for 10 min. The reaction is stopped by spotting aliquot
19、s of the reaction mixture onto Whatman P-81 phosphocellulose filter paper. The papers are then washed in 150 mM H3PO4, dried, and subjected to scintillation counting. The catalytic subunit of PKA is assayed by measuring 32Pphosphate incorporation into the substrate Kemptide (100 M). The activity of
20、CaMKII is determined by measuring phosphorylation of the synthetic peptide Autocamtide (100 M) in the presence of 100 M Calcium and 10 g/mL Calmodulin. A synthetic peptide analog of a fragment of neurogranin, NG(28-43) (10 M) is used as a specific substrate for the catalytic subunit of PKC. In all c
21、ases, substrate phosphorylation was linear with respect to time and enzyme concentration2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration 2Mice2 Adult male 129S3/SvImJ mice are used. In the 1-pairing paradigm of cue and contextual
22、 fear conditioning, animals are placed in the fear conditioning apparatus for 3 min, then a 30-sec acoustic conditioned stimulus (CS; white noise, 80 dB) is delivered. During the last second of the CS, a 1-sec shock unconditioned stimulus (US; 0.5 mA) is applied to the grid floor. To assess contextu
23、al learning, the animals are returned to the training context 24 hr post-training, and freezing behavior is scored for 5 min. To assess cue learning, the animals are placed in a different context (novel odor, lighting, cage floor, and visual cues) following contextual testing. Baseline behavior is m
24、easured for 3 min in the novel context (Pre-CS), then the tone is presented for 3 min. Freezing behavior is assessed with a time sampling procedure whereby the animal was observed for 1 sec every 5 sec. The experimenter is blind to drug treatment. Animals are injected with either vehicle (2 mL/kg, 1
25、00% DMSO) or SL327 (10, 30, and 50 mg/kg; at 2 mL/kg, dissolved in 100% DMSO) intraperitoneally 1 hr before training2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.客户使本产品发表的科研献See more customer validations on www.MedChemEREFERENCES1. Cheng Y, et al.
26、Current Development Status of MEK Inhibitors. Molecules. 2017 Sep 26;22(10). pii: E1551. Front Mol Neurosci. 2018 Aug 21;11:287. Brain Res Bull. 2016 Jun;124:40-TiplaxtininCat. No.: HY-15253CAS No.: 393105-53-8分式: CHFNO分量: 439.38作靶点: PAI-1作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 ye
27、arsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 54 mg/mL (122.90 mM)* “ means soluble, but saturation unknown.ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.2759 mL 11.3797 mL 22.7593 mL5 mM 0.4552 mL 2.2759 mL 4.5519 mL制备储备液10 mM 0.2276 mL 1.1380 mL 2.2759 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液BIO
28、LOGICAL ACTIVITY物活性 Tiplaxtinin 是种服有效的选择性的纤溶酶原激活物抑制剂-1 ( PAI-1) 抑制剂， IC50 为 2.7 M。IC 3 mg/kg Tiplaxtinin, 66.06.4 min; 10 mg/kg, 56.77.4 min; n=5-6; p0.05) and a reduced thrombus weight (control, 7.61.5 mg; 10 mg/kg Tiplaxtinin, 3.61.0 mg; p 90% corn oilSolubility: 2.5 mg/mL (2.88 mM); Clear solutio
29、n; Need warming1. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.88 mM); Suspended solution; Need ultrasonic and warming3. BIOLOGICAL ACTIVI
30、TY物活性 Venetoclax (ABT-199; GDC-0199) 是种效，有选择性和服活性的 Bcl-2 抑制剂， Ki 于0.01 nM。IC 11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P0.001) and tumor growth delay (TGD) of 26% (P0.05)1. Treatment of established xenografted (a mouse xenograft model of the T-ALL
31、 cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days resulted in a significant reduction of leukemic burden (P=0.0048)2.PROTOCOLCell Assay 1 RS4;11 cells are seeded at 50,000 per well in 96-well plates and treated with compounds diluted in half-log steps starting at 1 M and ending
32、 at 0.00005 M. All other leukemia and lymphoma cell lines are seeded at 15,000-20,000 cells per well in the appropriate medium and incubated with Venetoclax or Navitoclax for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression
33、 analysis of the concentration-response data. Mouse FL5.12-BCL-2 and FL5.12-BCL-XL cells are propagated and assessed. Bak-/- Bax-/- double knockout mouse embryonic fibroblasts are seeded into 96-well microtiter plates at 5,000 cells per well in DMEM supplemented with 10% FBS. Venetoclax (ABT-199) in
34、 the same culture medium is added in half-log dilutions starting at 5 M. The cells are then incubated at 37C (5% CO2) for 48 h, and the effects on proliferation are determined using Cell TiterGlo reagent1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.
35、Animal Administration 2Mice2 Nonobese diabetic/severe combined immunodeficient (NSG) mice are injected at 6 weeks of age in the tail vein with 150 L phosphate-buffered saline containing 5106 luciferase-labeled LOUCY cells. At regular time points, the bioluminescence is measured using the IVIS Lumina
36、 II imaging system. At 6 weeks, the cells are engrafted and the mice are randomly divided into 2 groups (with an equal number of males and females in both groups), and the treatment is started on day 0. Mice are treated with Venetoclax (ABT-199) 100 mg/kg body weight or with vehicle via oral gavage for 4 consecutive days. At days 0, 2, and 4 the bioluminescene is measured. Before imaging, the mi
