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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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. |
| 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 |
|
| 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 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
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