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Scriptaid

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names：
Scriptaid, HDAC inhibitor
CAS號(hào)：
287383-59-9
MDL Number： MFCD00386477
MF(分子式)： C18H18N2O4 MW(分子量)： 326
EINECS: Reaxys Number:
Pubchem ID:5186 Brand:BIOFOUNT

Scriptaid 是一種組蛋白去乙?；敢种苿?，在基于細(xì)胞的檢測(cè)中，最佳濃度為 6-8 μM，毒性低于曲古抑菌素 A，適用于多種生物系統(tǒng)。Scriptaid 可誘導(dǎo)結(jié)腸癌細(xì)胞的細(xì)胞周期停滯在培養(yǎng)和體外和體內(nèi)抑制腫瘤生長(zhǎng)。Scriptaid 還有助于克隆由體細(xì)胞核移植產(chǎn)生的近交小鼠品系。

貨品編碼	規(guī)格	純度	價(jià)格 (￥)	現(xiàn)價(jià)(￥)	特價(jià)(￥)	庫(kù)存描述	數(shù)量	總計(jì) (￥)
LSH65884-50mg	50mg	98%	￥ 4480.00	￥ 4480.00		1-3days	- +	￥ 0.00
LSH65884-10mg	10mg	98%	￥ 1180.00	￥ 1180.00		1-3days	- +	￥ 0.00

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中文別名	Scriptaid(287383-59-9);組蛋白去乙酰化酶 (HDAC) 抑制劑;HDAC抑制劑;組蛋白去乙?；敢种苿?Scriptide;GCK1026
英文別名	Scriptaid, HDAC inhibitor(287383-59-9);potent histone deacetylase (HDAC) inhibitor
CAS號(hào)	287383-59-9
Inchi	InChI=1S/C18H18N2O4/c21-15(19-24)10-2-1-3-11-20-17(22)13-8-4-6-12-7-5-9-14(16(12)13)18(20)23/h4-9,24H,1-3,10-11H2,(H,19,21)
InchiKey	JTDYUFSDZATMKU-UHFFFAOYSA-N
分子式 Formula	C18H18N2O4
分子量 Molecular Weight	326
溶解度Solubility
性狀	Solid,Powder
儲(chǔ)藏條件 Storage conditions	storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

體外研究

Scriptaid (6 μM) results in a >100-fold increase in histone acetylation in PANC-1 cell. Scriptaid (8 μM) is not lethal to PANC-1 cell and has limited effects (80% survival) on MDAMB-468. Scriptaid increases the transcription of pCMVb, p6SBE-luc and p6MBE-luc independent of a positive inducer of transcription. Scriptaid is capable of inducing high expression of p6MBE-luc, pCMVb, and pUB6/V5-LacZ, driven by viral (SV40 and CMV) or human (ubiquitin c, UB6) promoters, which do not depend on the specificity of the enhancer (SBE versus MBE), the type of promoter (viral versus cellular), the product of the reporter gene (luciferase versus b-gal), nor on the integration status of the reporter construct. Scriptaid induces high rates of somatic cell nuclear transfer (SCNT) oocytes development to the blastocyst stage and allowed full-term development (3.4, 4.2, 7.6, 6.8, and 4.1%) with all concentrations (50, 100, 250, 500, and 2000 nM respectively). Scriptaid improves the full-term development of cloned B6D2F1embryos in a dose-dependent manner with the maximum effect at 250 nM. Scriptaid enables the clone of all the important inbred mouse strains, such as C57BL/6, C3H/He, DBA/2, and 129/Sv. Scriptaid treatment enhances newly synthesized mRNA levels in cloned embryos. 250 nM Scriptaid treated for up to 48 h, does not inhibit the development of ICSI-fertilized embryos. Scriptaid inhibits T. gondii tachyzoite proliferation with IC50 of 39 nM. Scriptaid (0.225 μM) completely protects the HS68 monolayers from T. gondii tachyzoite.Scriptaid inhibits growth of ER negative cell lines, MDA-MB-231, MDA-MB-435 and Hs578t with IC50 of 0.5-1.0 μg/mL after 48 h treatment. 1 μg/ml Scriptaid treated for 48 h induces an accumulation of both acetylated H3 and acetylated H4 histone tail proteins, and a maximal of 20,000-fold increase of ER mRNA transcript. Scriptaid inhibits the proliferation and viability of the Ishikawa endometrial cancer cell line, and the SK-OV-3 ovarian cancer cell line with IC50 of 9 μM and 55 μM, respectively, while the normal human endometrial epithelial cells shows little sensitivity. Endometrial cancer cells and ovarian cancer cells cultured for 2 days in the presence of Scriptaid shows an accumulation in the G0/G1 phase (5 μM of Scriptaid) and G2/M phase (10 μM of Scriptaid) of the cell cycle, with a concomitant decrease in the proportion of those in the S phase. 10 μM of Scriptaid induces a 56.1% of apoptotic Ishikawa cells with loss of mitochondrial membrane potential, and decreased levels of cyclin A and bcl-2 levels by 50% and 20%, respectively.

體內(nèi)研究

Scriptaid elicits a dose-dependent decrease in lesion size (a maximal decrease of 45%) at 1.5 to 5.5 mg/kg and a concomitant attenuation in motor and cognitive deficits when delivered 30 minutes postinjury in a model of mode rate TBI. Comparable protection is achieved even when treatment is delayed to 12 h postinjury. The protection of motor and cognitive functions is long lasting, as similar improvements are detected 35 days postinjury. Scriptaid induces an increase in surviving neurons (42%), as well as the number/length of their processes within the CA3 region of the hippocampus and the pericontusional cortex. Scriptaid treatment prevents the decrease in phospho-AKT (p-AKT) and phosphorylated phosphatase and tensin homolog deleted on chromosome 10 ( p-PTEN) induced by TBI in cortical and CA3 hippocampal neurons. Scriptaid treatment (3.5 mg/kg) clearly inhibits tumor growth in a human breast cancer xenograft MDA-MB-231 model, reducing tumor volume by 75%.

產(chǎn)品說明	Scriptaid, 一種組蛋白去乙酰化酶 (HDAC) 抑制劑, 可用于癌癥研究?jī)H用于科學(xué)研究實(shí)驗(yàn)使用，不得用于其他用途
Introduction	Scriptaid, a potent histone deacetylase (HDAC) inhibitor, used in cancer research Only used for scientific research experiments, not for other purposes
Application1
Application2
Application3

警示圖
危險(xiǎn)性	warning
危險(xiǎn)性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H333吸入可能對(duì)身體有害
安全防護(hù)	P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P313獲得醫(yī)療建議/護(hù)理
備注	實(shí)驗(yàn)過程中防止吸入、食入，做好安全防護(hù)

1.Reduced Histone Deacetylase 7 Activity Restores Function to Misfolded CFTR in Cystic Fibrosis.（PMID 19966789)

2.Chemical Phylogenetics of Histone Deacetylases.(Nature Chemical Biology,PMID 20139990)

3. Lee, E.J., Lee, B.B., Kim, S.J., et al. Histone deacetylase inhibitor scriptaid induces cell cycle arrest and epigenetic change in colon cancer cells. Int. J. Oncol. 33, 767-776 (2008).

4. 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.

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