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Scriptaid (GCK-1026; Scriptide) 287383-59-9

Scriptaid (GCK-1026; Scriptide) 287383-59-9

CAS No.: 287383-59-9

Scriptaid (formerly GCK1026; Scriptide) is a novel and potent histone deacetylase (HDAC) inhibitor with potential antica
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Scriptaid (formerly GCK1026; Scriptide) is a novel and potent histone deacetylase (HDAC) inhibitor with potential anticancer activity. It exhibits strong in vitro anti-proliferative activity against a variety of cancer cell types, including ovarian cancer cell lines SK-OV-3 and endometrial cancer cell lines Ishikawa. Additionally, it may be able to treat lymphomas linked to the Epstein-Barr virus (EBV) by sensitizing the activity of antivirals.


Physicochemical Properties


Molecular Formula C18H18N2O4
Molecular Weight 326.35
Exact Mass 326.126
Elemental Analysis C, 66.25; H, 5.56; N, 8.58; O, 19.61
CAS # 287383-59-9
Related CAS #
287383-59-9
PubChem CID 5186
Appearance White to off-white solid powder
Density 1.3±0.1 g/cm3
Melting Point 160-161℃
Index of Refraction 1.646
LogP 0.43
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 6
Heavy Atom Count 24
Complexity 477
Defined Atom Stereocenter Count 0
SMILES

O=C1C2=C([H])C([H])=C([H])C3C([H])=C([H])C([H])=C(C(N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(N([H])O[H])=O)=O)C2=3

InChi Key JTDYUFSDZATMKU-UHFFFAOYSA-N
InChi Code

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)
Chemical Name

6-(1,3-dioxobenzo[de]isoquinolin-2-yl)-N-hydroxyhexanamide
Synonyms

GCK 1026; GCK-1026; GCK1026; Scriptaid; GCK1026
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets HDAC
ln Vitro

In vitro activity: Scriptaid (6 μM) causes a >100-fold increase in histone acetylation in PANC-1 cell. Scriptaid (8 μM) has minimal effects (80% survival rate) on MDAMB-468 but is not fatal to PANC-1 cells. Independent of a positive transcription inducer, scriptaid increases the transcription of pCMVb, p6SBE-luc, and p6MBE-luc. Using viral (SV40 and CMV) or human (ubiquitin c, UB6) promoters, Scriptaid can induce high expression of p6MBE-luc, pCMVb, and pUB6/V5-LacZ. This is independent of the reporter gene product (luciferase versus b-gal), the type of promoter (viral versus cellular), or the integration status of the reporter construct.[1] Scriptaid causes oocytes from somatic cell nuclear transfer (SCNT) to develop at high rates to the blastocyst stage. At all concentrations (50, 100, 250, 500, and 2000 nM, respectively), full-term development (3.4, 4.2, 7.6, 6.8, and 4.1%) is permitted. With a dose-dependent effect that peaks at 250 nM, scriptaid enhances the long-term development of cloned B6D2F1 embryos. The key inbred mouse strains, including DBA/2, C57BL/6, C3H/He, and 129/Sv, can all be cloned thanks to Scriptaid. Cloned embryos treated with Scriptaid have higher levels of newly synthesized mRNA. An ICSI-fertilized embryo's ability to develop is unaffected by a 48-hour exposure to 250 nM Scriptaid.[2] At an IC50 of 39 nM, scriptaid suppresses the growth of T. gondii tachyzoites. The HS68 monolayers are totally shielded from T. gondii tachyzoite by scriptaid (0.225 μM).[3] Scriptaid, after 48 hours of treatment, inhibits the growth of ER negative cell lines, MDA-MB-231, MDA-MB-435, and Hs578t, with an IC50 of 0.5-1.0 μg/mL. One microgram per milliliter After 48 hours of scriptaid treatment, ER mRNA transcript can increase by up to 20,000 times and both acetylated H3 and H4 histone tail proteins accumulate.[4] Scriptaid exhibits minimal sensitivity on normal human endometrial epithelial cells, but it inhibits the growth and viability of the Ishikawa endometrial cancer cell line and the SK-OV-3 ovarian cancer cell line with IC50 values of 9 μM and 55 μM, respectively. Cultured for two days in the presence of Scriptaid, endometrial and ovarian cancer cells exhibit an accumulation in the G0/G1 phase (5 μM of Scriptaid) and G2/M phase (10 μM of Scriptaid) of the cell cycle, accompanied by a decrease in the proportion of those in the S phase. Scriptaid at a concentration of 10 μM causes 56.1% of Ishikawa cells to undergo apoptosis, resulting in a loss of mitochondrial membrane potential and a 50% and 20% reduction in cyclin A and bcl-2 levels, respectively.[5]
ln Vivo
Scriptaid delivers 30 minutes post-injury and causes a dose-dependent reduction in lesion size (up to a maximum reduction of 45%), along with a concurrent attenuation of motor and cognitive deficits in a model of mode rate TBI. Treating an injury 12 hours after it occurs still results in comparable protection. As comparable gains are seen 35 days after the injury, the preservation of motor and cognitive abilities is long-lasting. In both the pericontusional cortex and the CA3 region of the hippocampus, scriptaid increases the number and length of surviving neurons (42%) as well as their relative numbers. The reduction in phospho-AKT (p-AKT) and phosphorylated phosphatase and tensin homolog deleted on chromosome 10 (p-PTEN) in cortical and CA3 hippocampal neurons caused by TBI is prevented by scriptaid treatment. [6] In a human breast cancer xenograft MDA-MB-231 model, scriptaid treatment (3.5 mg/kg) significantly inhibits tumor growth, resulting in a 75% reduction in tumor volume.[4]
Enzyme Assay Scriptaid (2 μg/mL) is added to PANC-1 cells and left them in culture medium for eighteen hours. Using trypsin-EDTA, treated and untreated cells are separated, rinsed in PBS, and then resuspended in a protein sample buffer. Reagents for the BCA protein assay measure the concentration of proteins. A 12% denaturing polyacrylamide gel is loaded with 50 μg of proteins from every sample. Then, using a MilliblotGraphite Electroblotter I, proteins are transferred to a nylon membrane. Rabbit antihuman acetyl-lysine antibody is incubated on the nylon membrane, and then it is developed using SuperSignal substrates, goat antirabbit antibody coupled with horseradish peroxidase, and film is used to detect the results.
Cell Assay The MTT assay is used to determine the IC50 concentrations of Scriptaid in MDA-MB-231, MDA-MB-435, and Hs578t cells. In order to conduct cell growth assays, MDA-MB-231, MDA-MB-435, and Hs578t cells are plated in 12-well plates at a density of 5000 cells per well. The cells are then treated with 1.0 µg/mL Scriptaid for a maximum of three days. A Coulter counter is used to count cells every day. Comparing treated and untreated cells yields the percent growth inhibition.
Animal Protocol
For the length of the studies, athymic female nude mice, aged four to six weeks, are kept under laminar flow hoods in an environmentally controlled, pathogen-free facility. MDA-MB-231 human breast cancer cells are injected into each flank of mice at a ratio of 2×106. The tumors are left untreated until they reach a diameter of about 0.1 cm3. After that, mice receive intraperitoneal injections of Scriptaid (3.5 µg/g mouse), TSA (0.5 µg/g mouse), or DMSO vehicle for five days in a row, with two days off per week, for a total of four weeks. Every week, the measurements of each individual tumor from each flank are recorded.
References

[1]. Cancer Res . 2000 Jun 15;60(12):3137-42.

[2]. Reproduction . 2009 Aug;138(2):309-17.

[3]. J Parasitol . 2007 Jun;93(3):694-700.

[4]. Breast Cancer Res Treat . 2003 Oct;81(3):177-86.

[5]. Int J Mol Med . 2006 Feb;17(2):323-9.

[6]. Neurotherapeutics . 2013 Jan;10(1):124-42.
Additional Infomation 6-(1,3-dioxo-2-benzo[de]isoquinolinyl)-N-hydroxyhexanamide is a member of isoquinolines.
Scriptaid is a histone deacetylase (HDAC) inhibitor researched for its anti-tumor properties.

Solubility Data


Solubility (In Vitro)
DMSO: 65~100 mg/mL (199.2~306.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.
Solubility in Formulation 2: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0642 mL 15.3210 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
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Is for research use only, not for human use. We do not sell to patients.