Scriptaid

製品コードS8043 別名:GCK 1026

Scriptaid 化学構造

分子量(MW):326.35

Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.

サイズ 価格(税別)  
JPY 36520.00
JPY 11620.00
JPY 28220.00

カスタマーフィードバック(1)

  • The relative expression of Oct4, Nanog, Klf4 and Sox2 at the blastocyst stage in ICSI-, ROSI- and ROSI + incubation of zygotes with 250 nM Scriptaid for 10 h (ROSI-S)-derived embryos. Five blastocysts in each pool were examined to obtain the data set in each column. Q-PCR analysis was performed in triplicate. Different letters indicate significant differences between values (P < 0.05).

    Human Reproduction, 2016, 1-12.. Scriptaid purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.
ターゲット
HDAC [1]
体外試験

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. [1] 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. [2] Scriptaid inhibits T. gondii tachyzoite proliferation with IC50 of 39 nM. Scriptaid (0.225 μM) completely protects the HS68 monolayers from T. gondii tachyzoite. [3] 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. [4] 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. [5]

体内試験 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. [6] 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%. [4]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Immunoblotting assay of histone acetylation:

PANC-1 cells are treated with 2 μg/mL of Scriptaid for 18 h in culture medium. Treated and untreated cells are harvested with trypsin-EDTA, washed with PBS, and resuspended in a protein sample buffer. Protein concentration is determined by BCA protein assay reagents. Fifty μg of proteins from each sample is loaded on a 12% denaturing polyacrylamide gel. Proteins are subsequently transferred to a nylon membrane using MilliblotGraphite Electroblotter I. The nylon membrane is incubated with rabbit antihuman acetyl-lysine antibody, followed by goat antirabbit antibody coupled to horseradish peroxidase, developed with SuperSignal substrates, and detected by film.
細胞試験: [4]
+ 展開
  • 細胞株: Human breast cancer cells MDA-MB-231
  • 濃度: ~10 μg/mL
  • 反応時間: 3 days
  • 実験の流れ: Cells are plated at a cell density of 5000 cells/well in 12 well plates and treated with Scriptaid for up to 3 days. Cells numbers are counted daily using a Coulter counter.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 動物モデル: Human breast carcinoma xenografts MDA-MB-231
  • 製剤: DMSO
  • 投薬量: 3.5 mg/kg
  • 投与方法: intraperitoneally for five consecutive days with 2 days rest each week for a total of 4 weeks
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 65 mg/mL (199.17 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
7mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 326.35
化学式

C18H18N2O4

CAS No. 287383-59-9
保管
in solvent
別名 GCK 1026

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HDACシグナル伝達経路

相関HDAC製品

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