Scriptaid

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Chemical Structure| 287383-59-9 同义名 : Scriptide;GCK1026
CAS号 : 287383-59-9
货号 : A120568
分子式 : C18H18N2O4
纯度 : 99%+
分子量 : 326.346
MDL号 : MFCD00386477
存储条件:

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(321.74 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

2% DMSO+30% PEG 300+2% Tween 80+water 7 mg/mL

生物活性
靶点
  • HDAC

描述 Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research. Scriptaid (1 µg/mL) treatment inhibits cell growth in breast cancer cell lines, results in increased accumulation of both acetyl H3 and acetyl H4 proteins in MDA-MB-231, MDA-MB-435, and Hs578t cells. Scriptaid also inhibits cell growth of MDA-MB-231, MDA-MB-435, and Hs578t cell lines, with IC50s of 0.5-1.0 µg/mL. Scriptaid (0.1-1.0 µg/mL) induces ER and PR mRNA expression in a dose dependent manner; when it is combined with AZA(5-aza-2'-deoxycytidine), they enhance ER expression and induce a functional ER protein (estrogen receptor alpha)[3]. Scriptaid and SAHA (suberoylanilide hydroxamic acid) 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 cells[4]. Scriptaid inhibited the growth of HeLa cells with IC50 of 2μM at 48h in a dose-dependent manner[5]. Treatment with 500nM scriptaid caused a significant increase in the acetylation of H3K9, H3K14, and H4K5. cEFs treated with 500nM. Scriptaid showed significantly decreased Gcn5, Hat1, Hdac6, and Bcl2 and increased Oct4 and Sox2 expression levels. Scriptaid affected the reprogramming of canine donor and cloned embryos, as well as early embryo development in canine-porcine iSCNT, by regulating reprogramming and apoptotic genes[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.32mL

3.06mL

1.53mL

30.64mL

6.13mL

3.06mL

参考文献

[1]Van Thuan N, Bui HT, et al. The histone deacetylase inhibitor scriptaid enhances nascent mRNA production and rescues full-term development in cloned inbred mice. Reproduction. 2009 Aug;138(2):309-17.

[2]Su GH, Sohn TA, et al. A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. Cancer Res. 2000 Jun 15;60(12):3137-42.

[3]Keen JC, Yan L, Mack KM, Pettit C, Smith D, Sharma D, Davidson NE. 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-aza 2'-deoxycytidine. Breast Cancer Res Treat. 2003 Oct;81(3):177-86

[4]Strobl JS, Cassell M, Mitchell SM, Reilly CM, Lindsay DS. 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

[5]Janaki Ramaiah M, Naushad SM, Lavanya A, Srinivas C, Anjana Devi T, Sampathkumar S, Dharan DB, Bhadra MP. Scriptaid cause 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

[6]No JG, Hur TY, Zhao M, Lee S, Choi MK, Nam YS, Yeom DH, Im GS, Kim DH. Scriptaid improves the reprogramming of donor cells and enhances canine-porcine interspecies embryo development. Reprod Biol. 2018 Mar;18(1):18-26