Scriptaid | CAS#287383-59-9 | HDAC inhibitor

MedKoo Cat#: 406810 | Name: Scriptaid

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Scriptaid, also known as GCK 1026, is a HDAC inhibitor. Scriptaid protects against traumatic brain injury via modulation of PTEN and AKT pathway. Scriptaid improves in vitro development and nuclear reprogramming of somatic cell nuclear transfer bovine embryos. Scriptaid enhances the response of human tumor cells to radiation. Scriptaid, induces glioma cell apoptosis through JNK activation and inhibits telomerase activity.

Chemical Structure

Scriptaid

CAS#287383-59-9

Theoretical Analysis

MedKoo Cat#: 406810

Name: Scriptaid

CAS#: 287383-59-9

Chemical Formula: C18H18N2O4

Exact Mass: 326.1267

Molecular Weight: 326.35

Elemental Analysis: C, 66.25; H, 5.56; N, 8.58; O, 19.61

Price and Availability

Size	Price	Availability
100mg	USD 550.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,150.00	2 Weeks
2g	USD 3,850.00	2 Weeks
5g	USD 5,650.00	2 Weeks

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Related CAS #

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Synonym

GCK 1026; GCK-1026; GCK1026; Scriptaid

IUPAC/Chemical Name

N-hydroxy-1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-hexananmide

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)

SMILES Code

O=C(NO)CCCCCN(C(C1=CC=CC2=CC=CC3=C12)=O)C3=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Scriptaid is a potent HDAC inhibitor, is a sensitizer to antivirals, and has potential for Epstein Barr virus (EBV)-associated lymphomas treatment.

In vitro activity:

Scriptaid is a potential anti-cancer drug, either alone or in combination with zebularine, for breast cancer treatment. MDA-MB-231 cells exhibited a significant reduction in cell migration after the combination of scriptaid and zebularine. Scriptaid and the combination induced cell cycle arrest at the G0/G1 phase. All treatments induced apoptotic features in both cell lines. Reference: Anticancer Agents Med Chem. 2022;22(8):1582-1591. https://pubmed.ncbi.nlm.nih.gov/34102995/

In vivo activity:

Scriptaid is a potential treatment for brain injury after intracranial hemorrhage (ICH). In a mouse model of ICH model, Scriptaid reduced neurological deficits, brain atrophy, and white matter injury in a dose-dependent manner. Scriptaid also decreased the expression of pro-inflammatory cytokines IL1β and TNFα, as well as iNOS, after ICH. Reference: CNS Neurol Disord Drug Targets. 2020;19(1):55-65. https://pubmed.ncbi.nlm.nih.gov/31858907/

	Solvent	mg/mL	mM
Solubility
	DMF	3.0	9.19
	DMSO	2.5	7.66

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 326.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yap ZH, Kong WY, Azeez AR, Fang CM, Ngai SC. Anti-Cancer Effects of Epigenetics Drugs Scriptaid and Zebularine in Human Breast Adenocarcinoma Cells. Anticancer Agents Med Chem. 2022;22(8):1582-1591. doi: 10.2174/1871520621666210608103251. PMID: 34102995. 2. Sun N, Uda Y, Azab E, Kochen A, Santos RNCE, Shi C, Kobayashi T, Wein MN, Divieti Pajevic P. Effects of histone deacetylase inhibitor Scriptaid and parathyroid hormone on osteocyte functions and metabolism. J Biol Chem. 2019 Jun 21;294(25):9722-9733. doi: 10.1074/jbc.RA118.007312. Epub 2019 May 8. PMID: 31068415; PMCID: PMC6597811. 3. Yang H, Gao X, Su J, Jiang H, Lei Y, Ni W, Gu Y. Pharmacokinetics and Acute Toxicity of a Histone Deacetylase Inhibitor, Scriptaid, and its Neuroprotective Effects in Mice After Intracranial Hemorrhage. CNS Neurol Disord Drug Targets. 2020;19(1):55-65. doi: 10.2174/1871527319666191220111126. PMID: 31858907. 4. Meng Q, Yang G, Yang Y, Ding F, Hu F. Protective effects of histone deacetylase inhibition by Scriptaid on brain injury in neonatal rat models of cerebral ischemia and hypoxia. Int J Clin Exp Pathol. 2020 Feb 1;13(2):179-191. PMID: 32211098; PMCID: PMC7061803.

In vitro protocol:

In vivo protocol:

1. Yang H, Gao X, Su J, Jiang H, Lei Y, Ni W, Gu Y. Pharmacokinetics and Acute Toxicity of a Histone Deacetylase Inhibitor, Scriptaid, and its Neuroprotective Effects in Mice After Intracranial Hemorrhage. CNS Neurol Disord Drug Targets. 2020;19(1):55-65. doi: 10.2174/1871527319666191220111126. PMID: 31858907. 2. Meng Q, Yang G, Yang Y, Ding F, Hu F. Protective effects of histone deacetylase inhibition by Scriptaid on brain injury in neonatal rat models of cerebral ischemia and hypoxia. Int J Clin Exp Pathol. 2020 Feb 1;13(2):179-191. PMID: 32211098; PMCID: PMC7061803.

1: Liang S, Zhao MH, Choi JW, Kim NH, Cui XS. Scriptaid Treatment Decreases DNA Methyltransferase 1 Expression by Induction of MicroRNA-152 Expression in Porcine Somatic Cell Nuclear Transfer Embryos. PLoS One. 2015 Aug 11;10(8):e0134567. doi: 10.1371/journal.pone.0134567. eCollection 2015. PubMed PMID: 26261994; PubMed Central PMCID: PMC4532471. 2: Sun H, Lu F, Zhu P, Liu X, Tian M, Luo C, Ruan Q, Ruan Z, Liu Q, Jiang J, Wei Y, Shi D. Effects of Scriptaid on the Histone Acetylation, DNA Methylation and Development of Buffalo Somatic Cell Nuclear Transfer Embryos. Cell Reprogram. 2015 Oct;17(5):404-14. doi: 10.1089/cell.2014.0084. Epub 2015 Jun 2. PubMed PMID: 26035741. 3: Berghauser Pont LM, Kleijn A, Kloezeman JJ, van den Bossche W, Kaufmann JK, de Vrij J, Leenstra S, Dirven CM, Lamfers ML. The HDAC Inhibitors Scriptaid and LBH589 Combined with the Oncolytic Virus Delta24-RGD Exert Enhanced Anti-Tumor Efficacy in Patient-Derived Glioblastoma Cells. PLoS One. 2015 May 18;10(5):e0127058. doi: 10.1371/journal.pone.0127058. eCollection 2015. PubMed PMID: 25993039; PubMed Central PMCID: PMC4436250. 4: Sun H, Lu F, Liu X, Tian M, Ruan Z, Zhu P, Ruan Q, Jiang J, Shi D. Effects of scriptaid on the histone acetylation of buffalo oocytes and their ability to support the development of somatic cell nuclear transfer embryos. Theriogenology. 2015 Apr 15;83(7):1219-25. doi: 10.1016/j.theriogenology.2015.01.003. Epub 2015 Jan 8. PubMed PMID: 25640327. 5: Zhang H, Wang Y, Sang Y, Zhang Y, Hua S. Combination of S-adenosylhomocysteine and scriptaid, a non-toxic epigenetic modifying reagent, modulates the reprogramming of bovine somatic-cell nuclear transfer embryos. Mol Reprod Dev. 2014 Jan;81(1):87-97. doi: 10.1002/mrd.22287. Epub 2013 Dec 17. PubMed PMID: 24347442. 6: Wen BQ, Li J, Li JJ, Tian SJ, Sun SC, Qi X, Cai WT, Chang QL. The histone deacetylase inhibitor Scriptaid improves in vitro developmental competence of ovine somatic cell nuclear transferred embryos. Theriogenology. 2014 Jan 15;81(2):332-9. doi: 10.1016/j.theriogenology.2013.09.032. Epub 2013 Oct 6. PubMed PMID: 24182741. 7: Xiong X, Lan D, Li J, Zhong J, Zi X, Ma L, Wang Y. Zebularine and scriptaid significantly improve epigenetic reprogramming of yak fibroblasts and cloning efficiency. Cell Reprogram. 2013 Aug;15(4):293-300. doi: 10.1089/cell.2012.0092. Epub 2013 Jun 22. PubMed PMID: 23790013. 8: Chen CH, Du F, Xu J, Chang WF, Liu CC, Su HY, Lin TA, Ju JC, Cheng WT, Wu SC, Chen YE, Sung LY. Synergistic effect of trichostatin A and scriptaid on the development of cloned rabbit embryos. Theriogenology. 2013 Jun;79(9):1284-93. doi: 10.1016/j.theriogenology.2013.03.003. Epub 2013 Apr 6. PubMed PMID: 23566670; PubMed Central PMCID: PMC3677057. 9: Gómez MC, Biancardi MN, Jenkins JA, Dumas C, Galiguis J, Wang G, Earle Pope C. Scriptaid and 5-aza-2'deoxycytidine enhanced expression of pluripotent genes and in vitro developmental competence in interspecies black-footed cat cloned embryos. Reprod Domest Anim. 2012 Dec;47 Suppl 6:130-5. doi: 10.1111/rda.12027. PubMed PMID: 23279482. 10: Wang G, Jiang X, Pu H, Zhang W, An C, Hu X, Liou AK, Leak RK, Gao Y, Chen J. Scriptaid, a novel histone deacetylase inhibitor, protects against traumatic brain injury via modulation of PTEN and AKT pathway : scriptaid protects against TBI via AKT. Neurotherapeutics. 2013 Jan;10(1):124-42. doi: 10.1007/s13311-012-0157-2. PubMed PMID: 23132328; PubMed Central PMCID: PMC3557358. 11: Abaza MS, Bahman AM, Al-Attiyah RJ, Kollamparambil AM. Synergistic induction of apoptosis and chemosensitization of human colorectal cancer cells by histone deacetylase inhibitor, scriptaid, and proteasome inhibitors: potential mechanisms of action. Tumour Biol. 2012 Dec;33(6):1951-72. doi: 10.1007/s13277-012-0456-6. Epub 2012 Jul 19. PubMed PMID: 23011889. 12: Mao J, Tessanne K, Whitworth KM, Spate LD, Walters EM, Samuel MS, Murphy CN, Tracy L, Zhao J, Prather RS. Effects of combined treatment of MG132 and scriptaid on early and term development of porcine somatic cell nuclear transfer embryos. Cell Reprogram. 2012 Oct;14(5):385-9. doi: 10.1089/cell.2012.0018. Epub 2012 Aug 23. PubMed PMID: 22917492; PubMed Central PMCID: PMC3459054. 13: Giacinti L, Giacinti C, Gabellini C, Rizzuto E, Lopez M, Giordano A. Scriptaid effects on breast cancer cell lines. J Cell Physiol. 2012 Oct;227(10):3426-33. doi: 10.1002/jcp.24043. PubMed PMID: 22213035. 14: Panda SK, George A, Saha A, Sharma R, Singh AK, Manik RS, Chauhan MS, Palta P, Singla SK. Effect of scriptaid, a histone deacetylase inhibitor, on the developmental competence of Handmade cloned buffalo (Bubalus bubalis) embryos. Theriogenology. 2012 Jan 1;77(1):195-200. doi: 10.1016/j.theriogenology.2011.07.033. Epub 2011 Sep 14. PubMed PMID: 21924478. 15: Wang LJ, Zhang H, Wang YS, Xu WB, Xiong XR, Li YY, Su JM, Hua S, Zhang Y. Scriptaid improves in vitro development and nuclear reprogramming of somatic cell nuclear transfer bovine embryos. Cell Reprogram. 2011 Oct;13(5):431-9. doi: 10.1089/cell.2011.0024. Epub 2011 Jul 20. PubMed PMID: 21774687. 16: Whitworth KM, Zhao J, Spate LD, Li R, Prather RS. Scriptaid corrects gene expression of a few aberrantly reprogrammed transcripts in nuclear transfer pig blastocyst stage embryos. Cell Reprogram. 2011 Jun;13(3):191-204. doi: 10.1089/cell.2010.0087. Epub 2011 May 6. PubMed PMID: 21548827. 17: Ying H, Zhang Y, Lin S, Han Y, Zhu HZ. Histone deacetylase inhibitor Scriptaid reactivates latent HIV-1 promoter by inducing histone modification in in vitro latency cell lines. Int J Mol Med. 2010 Aug;26(2):265-72. PubMed PMID: 20596607. 18: Kuribayashi T, Ohara M, Sora S, Kubota N. Scriptaid, a novel histone deacetylase inhibitor, enhances the response of human tumor cells to radiation. Int J Mol Med. 2010 Jan;25(1):25-9. PubMed PMID: 19956898. 19: Sharma V, Koul N, Joseph C, Dixit D, Ghosh S, Sen E. HDAC inhibitor, scriptaid, induces glioma cell apoptosis through JNK activation and inhibits telomerase activity. J Cell Mol Med. 2010 Aug;14(8):2151-61. doi: 10.1111/j.1582-4934.2009.00844.x. Epub 2010 Jul 6. PubMed PMID: 19583803; PubMed Central PMCID: PMC3823006. 20: Van Thuan N, Bui HT, Kim JH, Hikichi T, Wakayama S, Kishigami S, Mizutani E, Wakayama T. 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. doi: 10.1530/REP-08-0299. Epub 2009 May 11. PubMed PMID: 19433501.