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Scriptaid {[allProObj[0].p_purity_real_show]}

货号:A120568 同义名: Scriptide; GCK1026

Scriptaid是一种 HDAC 抑制剂,对乙酰化 H4 有更强的抑制作用。

Scriptaid 化学结构 CAS号:287383-59-9
Scriptaid 化学结构
CAS号:287383-59-9
Scriptaid 3D分子结构
CAS号:287383-59-9
Scriptaid 化学结构 CAS号:287383-59-9
Scriptaid 3D分子结构 CAS号:287383-59-9
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Scriptaid 纯度/质量文件 产品仅供科研

货号:A120568 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-A, IC50: 16 nM

HD1-B, IC50: 7.5 nM

+++

HD2, IC50: 10 nM

99%+
MC1568 ++

HD1-A (Maize), IC50: 100 nM

HD1-B (Maize), IC50: 3.4 μM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

99%+
Scriptaid 99%+
Valproic acid sodium Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

99%+
Dacinostat +++

HDAC, IC50: 32 nM

98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC8, IC50: 79.8 nM

++

HDAC9, IC50: 67.2 nM

HER2,EGFR 99%+
M344 ++

HDAC, IC50: 100 nM

99%+
Splitomicin +

Sir2p, IC50: 60 μM

99%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%+
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%+
Parthenolide p53,NF-κB 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%+
Tasquinimod 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

99%+
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

99%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%+
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

99%+
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

++++

HDAC10, IC50: 0.46 nM

++++

HDAC11, IC50: 0.37 nM

++++

HDAC2, IC50: 0.33 nM

++++

HDAC3, IC50: 4.86 nM

++++

HDAC4, IC50: 0.64 nM

++++

HDAC5, IC50: 3.69 nM

++++

HDAC8, IC50: 4.26 nM

97%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99%+
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

99%+
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++

HDAC2, IC50: 96 nM

+++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC8, IC50: 140 nM

++

HDAC9, IC50: 70 nM

99%+
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Scriptaid 生物活性

靶点
  • HDAC

描述 Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research. Scriptaid (1 µg/mL) treatment inhibits cell growth in breast cancer cell lines, results in increased accumulation of both acetyl H3 and acetyl H4 proteins in MDA-MB-231, MDA-MB-435, and Hs578t cells. Scriptaid also inhibits cell growth of MDA-MB-231, MDA-MB-435, and Hs578t cell lines, with IC50s of 0.5-1.0 µg/mL. Scriptaid (0.1-1.0 µg/mL) induces ER and PR mRNA expression in a dose dependent manner; when it is combined with AZA(5-aza-2'-deoxycytidine), they enhance ER expression and induce a functional ER protein (estrogen receptor alpha)[3]. Scriptaid and SAHA (suberoylanilide hydroxamic acid) preferentially inhibit the Class I histone deacetylases, hdac1, 2, and 3. Scriptaid is a potent anti-T. gondii compound with low cytotoxicity, and the IC50 is 39 nM. Scriptaid has atypical effects in T. gondiiinfected HS68 cells[4]. Scriptaid inhibited the growth of HeLa cells with IC50 of 2μM at 48h in a dose-dependent manner[5]. Treatment with 500nM scriptaid caused a significant increase in the acetylation of H3K9, H3K14, and H4K5. cEFs treated with 500nM. Scriptaid showed significantly decreased Gcn5, Hat1, Hdac6, and Bcl2 and increased Oct4 and Sox2 expression levels. Scriptaid affected the reprogramming of canine donor and cloned embryos, as well as early embryo development in canine-porcine iSCNT, by regulating reprogramming and apoptotic genes[6].

Scriptaid 细胞实验

Cell Line
Concentration Treated Time Description References
Huh7 cells 10 µM 24 hours Enhance fenretinide-induced apoptosis Hepatology. 2011 Mar;53(3):865-74.
GM979 cells 2 µM 4 days Scriptaid induced γ gene promoter activity by 2.6-fold Blood. 2004 Jan 15;103(2):701-9.
HepG2 cells 10 µM 24 hours Sensitize HepG2 cells to fenretinide-induced apoptosis Hepatology. 2011 Mar;53(3):865-74.
Hep3B cells 10 µM 24 hours Enhance fenretinide-induced apoptosis Hepatology. 2011 Mar;53(3):865-74.
Human BFUe cells 5 µM 14 days Scriptaid increased γ/γ + β mRNA ratio by 3.27-fold in BFUe cultures Blood. 2004 Jan 15;103(2):701-9.
Porcine SCNT embryos 500 nM 15 hours Evaluate the effect of combined Scriptaid and DRB treatment on transcriptional activity in SCNT embryos, results showed combined treatment significantly inhibited transcriptional activity. Int J Mol Sci. 2022 Nov 16;23(22):14142.
Porcine fetal fibroblasts (PFF) 500 nM 15 hours Evaluate the effect of Scriptaid on transcriptional activity, results showed Scriptaid alone did not affect transcriptional activity. Int J Mol Sci. 2022 Nov 16;23(22):14142.
Human pulmonary artery endothelial cells (HPAECs) 8 µM 24 hours Induced expression of extracellular superoxide dismutase (EC-SOD) up to 10-fold, whereas expression of the prooxidant gene NADPH oxidase 4 was decreased by more than 95%. We also found that this differential regulation of anti- and prooxidant gene expression resulted in significant attenuation in the cellular levels of reactive oxygen species. Modulation of Extracellular Superoxide Dismutase and NOX4 Expression Using Histone Deacetylase Class I Inhibitors. Am J Respir Cell Mol Biol.
Oligodendrocytes 1 µM 24 hours Scriptaid provides protection to oligodendrocytes treated with microglial conditioned medium Proc Natl Acad Sci U S A. 2015 Mar 3;112(9):2853-8.
UM-HACC-2A cells 10 µM 24 hours Scriptaid effectively inhibited Snail expression, induced hyperacetylation of histone H3K9, reduced cell migration, and effectively disrupted tumorspheres. Int J Mol Sci. 2024 Jan 29;25(3):1646.
T98G 5-20 µM 24 hours Scriptaid reduced glioma cell viability by increasing JNK activation and induced apoptosis. J Cell Mol Med. 2010 Aug;14(8):2151-61.
LN229 5-20 µM 24 hours Scriptaid reduced glioma cell viability by increasing JNK activation and induced apoptosis. J Cell Mol Med. 2010 Aug;14(8):2151-61.
A375 cells 1 µM 3 hours Evaluate G4 stabilization and DNA damage response of Scriptaid in melanoma cells, results showed Scriptaid significantly stabilized G4s and induced DNA damage Open Biol. 2025 Feb;15(2):240183.
Rat aortic SMC 6 µM 30 minutes Inhibited mitogen-induced SMC proliferation by preventing Rb protein phosphorylation and cell cycle G1→S phase progression Arterioscler Thromb Vasc Biol. 2011 Apr;31(4):851-60.
Microglia 1 µM 48 hours Scriptaid indirectly protects oligodendrocytes by modulating microglial polarization and reducing inflammatory responses Proc Natl Acad Sci U S A. 2015 Mar 3;112(9):2853-8.
HEK293 tau-BiFC cells 3 µM 48 hours To evaluate the effect of Scriptaid on tau aggregation, results showed that Scriptaid significantly increased tau-BiFC fluorescence intensity, indicating increased tau aggregation. Int J Mol Sci. 2019 Sep 1;20(17):4283.
CRL1790 cells 128.8 µM (IC50) 48 hours Evaluate cytotoxic activity of Scriptaid in non-tumoral colon epithelial cells, results showed Scriptaid induced cytotoxicity Open Biol. 2025 Feb;15(2):240183.
HCT116 cells 42.8 µM (IC50) 48 hours Evaluate cytotoxic activity of Scriptaid in colorectal cancer cells, results showed Scriptaid induced cytotoxicity Open Biol. 2025 Feb;15(2):240183.
HT29 cells 8.9 µM (IC50) 48 hours Evaluate cytotoxic activity of Scriptaid in colorectal cancer cells, results showed Scriptaid induced cytotoxicity Open Biol. 2025 Feb;15(2):240183.
SW480 cells 9.6 µM (IC50) 48 hours Evaluate cytotoxic activity of Scriptaid in colorectal cancer cells, results showed Scriptaid induced cytotoxicity Open Biol. 2025 Feb;15(2):240183.
U87 cells 3.2 µM 48 hours or 72 hours To verify whether Scriptaid could enhance the inhibitory effect of temozolomide on U87 cell proliferation. Results showed that Scriptaid combined with temozolomide significantly inhibited U87 cell proliferation. Front Immunol. 2025 Jan 21;15:1523034.
Primary microglia 1 µM 6 hours Scriptaid modulated microglia polarization, reduced pro-inflammatory cytokine secretion, and protected oligodendrocytes from hemoglobin-induced injury. J Cereb Blood Flow Metab. 2021 May;41(5):958-974.
Human breast CAFs (hCAFs) 10 µM 7 days To study the reversal effect of Scriptaid on CAF marker expression. Results showed Scriptaid reduced the expression of SMA, fibronectin, col1, and palladin. Br J Cancer. 2018 May;118(10):1359-1368.
Murine melanoma CAFs (mCAFs) 10 µM 7 days To study the reversal effect of Scriptaid on CAF marker expression. Results showed Scriptaid reduced the expression of SMA, fibronectin, col1, and palladin. Br J Cancer. 2018 May;118(10):1359-1368.

Scriptaid 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 J mice Controlled cortical impact (CCI) model Intraperitoneal injection 1.5 to 5.5 mg/kg Administered at 30 minutes or 12 hours post-injury, continued for 3 days Scriptaid, when administered at 30 minutes or 12 hours post-injury, significantly reduced lesion volume and attenuated motor and cognitive deficits. Additionally, Scriptaid modulated the PTEN and AKT pathways, increasing the number of surviving neurons and the number/length of their processes in the CA3 region of the hippocampus and the pericontusional cortex. Neurotherapeutics. 2013 Jan;10(1):124-42
Mice Traumatic brain injury model Intraperitoneal injection 3.5 mg/kg Injected at 2, 26, and 50 hours post-injury Scriptaid protects white matter integrity by modulating microglial polarization and reducing inflammation Proc Natl Acad Sci U S A. 2015 Mar 3;112(9):2853-8.
C57BL/6 male mice ICH model Intraperitoneal injection 3.5 mg/kg Administered at 2, 26, and 50 hours post-ICH Scriptaid improved neurological functional recovery, reduced white matter injury, and alleviated neuroinflammation by modulating microglia/macrophage polarization after ICH. J Cereb Blood Flow Metab. 2021 May;41(5):958-974.
C57BL/6J mice Vascular injury model Intraperitoneal injection 3.5 μg/g The day before injury, on the day of the injury, and every other day thereafter for 28 days Reduced neointima formation and cyclin D1 expression following vascular injury Arterioscler Thromb Vasc Biol. 2011 Apr;31(4):851-60.
Mice B16F10 melanoma model Intraperitoneal injection 5.5 mg/kg 3 times per week until the end of the experiment To study the effect of Scriptaid on tumor growth and CAF abundance. Results showed Scriptaid inhibited tumor growth by approximately twofold and significantly reduced the number of SMA+/Col1+ CAFs. Br J Cancer. 2018 May;118(10):1359-1368.
Pigs SCNT embryo transfer model In vitro culture followed by transfer 500 nM Scriptaid + 100 µM DRB Single treatment, lasting 15 hours Evaluate the effect of combined Scriptaid and DRB treatment on SCNT embryo development, results showed combined treatment promoted normal fetal development and production of healthy cloned piglets. Int J Mol Sci. 2022 Nov 16;23(22):14142.

Scriptaid 参考文献

[1]Van Thuan N, Bui HT, et al. 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.

[2]Su GH, Sohn TA, et al. A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. Cancer Res. 2000 Jun 15;60(12):3137-42.

[3]Keen JC, Yan L, Mack KM, Pettit C, Smith D, Sharma D, Davidson NE. A novel histone deacetylase inhibitor, scriptaid, enhances expression of functional estrogen receptor alpha (ER) in ER negative human breast cancer cells in combination with 5-aza 2'-deoxycytidine. Breast Cancer Res Treat. 2003 Oct;81(3):177-86

[4]Strobl JS, Cassell M, Mitchell SM, Reilly CM, Lindsay DS. Scriptaid and suberoylanilide hydroxamic acid are histone deacetylase inhibitors with potent anti-Toxoplasma gondii activity in vitro. J Parasitol. 2007 Jun;93(3):694-700

[5]Janaki Ramaiah M, Naushad SM, Lavanya A, Srinivas C, Anjana Devi T, Sampathkumar S, Dharan DB, Bhadra MP. Scriptaid cause histone deacetylase inhibition and cell cycle arrest in HeLa cancer cells: A study on structural and functional aspects. Gene. 2017 Sep 5;627:379-386

[6]No JG, Hur TY, Zhao M, Lee S, Choi MK, Nam YS, Yeom DH, Im GS, Kim DH. Scriptaid improves the reprogramming of donor cells and enhances canine-porcine interspecies embryo development. Reprod Biol. 2018 Mar;18(1):18-26

Scriptaid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.32mL

3.06mL

1.53mL

30.64mL

6.13mL

3.06mL

Scriptaid 技术信息

CAS号287383-59-9
分子式C18H18N2O4
分子量 326.35
SMILES Code O=C(NO)CCCCCN(C(C1=CC=CC2=CC=CC3=C12)=O)C3=O
MDL No. MFCD00386477
别名 Scriptide; GCK1026
运输蓝冰
InChI Key JTDYUFSDZATMKU-UHFFFAOYSA-N
Pubchem ID 5186
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 105 mg/mL(321.74 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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