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Scriptaid

別名：GCK 1026

Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.

Scriptaid 化学構造

CAS No. 287383-59-9

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JPY 22000 国内在庫あり
JPY 44500 国内在庫なし(納期7~10日)

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Scriptaid 関連製品

シグナル伝達経路

HDAC Signaling Pathways

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

生物活性

製品説明 Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.
Targets
HDAC [1]
In Vitro
In vitro Scriptaid (6 μM) results in a >100-fold increase in histone acetylation in PANC-1 cell. This compound (8 μM) is not lethal to PANC-1 cell and has limited effects (80% survival) on MDAMB-468. It increases the transcription of pCMVb, p6SBE-luc and p6MBE-luc independent of a positive inducer of transcription. This chemical 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] It 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). This compound improves the full-term development of cloned B6D2F1embryos in a dose-dependent manner with the maximum effect at 250 nM. It enables the clone of all the important inbred mouse strains, such as C57BL/6, C3H/He, DBA/2, and 129/Sv. This chemical treatment enhances newly synthesized mRNA levels in cloned embryos. 250 nM of this compound treated for up to 48 h, does not inhibit the development of ICSI-fertilized embryos. [2] It inhibits T. gondii tachyzoite proliferation with IC50 of 39 nM. This compound (0.225 μM) completely protects the HS68 monolayers from T. gondii tachyzoite. [3] It 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 of this compound 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] It 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 this compound shows an accumulation in the G0/G1 phase (5 μM of this chemical) and G2/M phase (10 μM of this compound) of the cell cycle, with a concomitant decrease in the proportion of those in the S phase. 10 μM of this chemical 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]
Kinase Assay 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.
細胞実験 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.
In Vivo
In Vivo 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. This compound 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. This 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] This chemical (3.5 mg/kg) clearly inhibits tumor growth in a human breast cancer xenograft MDA-MB-231 model, reducing tumor volume by 75%. [4]
動物実験 動物モデル Human breast carcinoma xenografts MDA-MB-231
投与量 3.5 mg/kg
投与経路 intraperitoneally for five consecutive days with 2 days rest each week for a total of 4 weeks
  • https://pubmed.ncbi.nlm.nih.gov/10866300/
  • https://pubmed.ncbi.nlm.nih.gov/19433501/
  • https://pubmed.ncbi.nlm.nih.gov/17626366/
  • https://pubmed.ncbi.nlm.nih.gov/14620913/
  • https://pubmed.ncbi.nlm.nih.gov/16391833/
  • https://pubmed.ncbi.nlm.nih.gov/23132328/

化学情報

分子量 326.35 化学式

C18H18N2O4
CAS No. 287383-59-9 SDF Download Scriptaid SDFをダウンロードする
Smiles C1=CC2=C3C(=C1)C(=O)N(C(=O)C3=CC=C2)CCCCCC(=O)NO
保管

In vitro
Batch:

DMSO : 65 mg/mL ( (199.17 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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