Scriptaid
(Synonyms: Scriptide; GCK1026) 目录号 : GC15315HDAC inhibitor
Cas No.:287383-59-9
Sample solution is provided at 25 µL, 10mM.
Scriptaid, identified by a high-throughput transcriptional screening, is a novel histone deacetylase (HDAC) with specific potency towards class I HDACs (50% inhibition concentration IC50 values of 0.6 μM for HDAC1 and HDAC3 and 1 μM for HDAC8). Scriptaid shares a similar chemical structure with several others hydroxamic acid-containing HDAC inhibitors (such as TSA and nullscript), which consists of a hydroxamic acid group, an aliphatic chain and an aromatic cap at the other end. Scriptaid has the potential to be used for the treatment of glioblastoma multiforme (GBM), one of the most challenging solid cancers to treat, for its ability to induce apoptosis in glioblastoma cells.
Reference
Sharma V, Koul N, Joseph C, Dixit D, Ghosh S, Sen E. HDAC inhibitor, scriptaid, induces glioma cell apoptosis through JNK activation and inhibits telomerase activity. J Cell Mol Med. 2010;14(8):2151-2161.
Hu E, Dul E, Sung CM, Chen Z, Kirkpatrick R, Zhang GF, Johanson K, Liu R, Lago A, Hofmann G, Macarron R, de los Frailes M, Perez P, Krawiec J, Winkler J, Jaye M. Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther. 2003;307(2):720-728.
Su GH, Sohn TA, Ryu B, Kern SE. A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. Cancer Res. 2000; 60(12):3137-3142.
Cell experiment [1]: | |
Cell lines |
MDA-MB-231 cell lines |
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions |
48 h; 1.0 mg/mL |
Applications |
Based on MTT assay a concentration of 1mg/ml of Scriptaid was chosen for the experiments in MDA-MB-231. MDA-MB-231 cells were treated with 0.1, 0.5, and 1.0 mg/mL of Scriptaid for 48 h. A dose-dependent increase in α-ER mRNA was detectable with concentrations as low as 0.1mg/ml in MDA-MB-231. Maximal α-ER mRNA was detected at 1.0mg/ml. |
Animal experiment [2]: | |
Animal models |
B6D2F1 male and female mice; SCNT embryos |
Dosage form |
250 nM; immersion |
Applications |
Treating SCNT embryos with HDAC inhibitor, scriptaid, all the important inbred mouse strains can be cloned, such as C57BL/6, C3H/He, DBA/2, and 129/Sv. Normal development, reproductive ability, and genotype in cloned inbred mice produced by scriptaid treatment. Scriptaid has also lower toxicity for embryo development that treatment of ICSI-fertilized embryos with 250 nM scriptaid, for up to 48 h, did not inhibit in vitro or in vivo development. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Giacinti L, Giacinti C, Gabellini C, et al. Scriptaid effects on breast cancer cell lines[J]. Journal of cellular physiology, 2012, 227(10): 3426-3433. [2] Van Thuan N, Bui H T, Kim J H, et al. The histone deacetylase inhibitor scriptaid enhances nascent mRNA production and rescues full-term development in cloned inbred mice[J]. Reproduction, 2009, 138(2): 309-317. |
Cas No. | 287383-59-9 | SDF | |
别名 | Scriptide; GCK1026 | ||
化学名 | 6-(1,3-dioxobenzo[de]isoquinolin-2-yl)-N-hydroxyhexanamide | ||
Canonical SMILES | C1=CC2=C3C(=C1)C(=O)N(C(=O)C3=CC=C2)CCCCCC(=O)NO | ||
分子式 | C18H18N2O4 | 分子量 | 326.35 |
溶解度 | ≥ 13.1 mg/mL in DMSO, ≥ 3.17 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
General tips | 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0642 mL | 15.321 mL | 30.6419 mL |
5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL |
10 mM | 0.3064 mL | 1.5321 mL | 3.0642 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet