Trichostatin A is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM and HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
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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 |
EGFR,HER2 | 99%+ | ||||||
M344 |
++
HDAC, IC50: 100 nM |
99%+ | |||||||||||||||||
Splitomicin |
+
Sir2p, IC50: 60 μM |
95% | |||||||||||||||||
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 |
98% | ||||||||||||||||
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 |
99+% | ||||||||||
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 | HDACs are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC11)[1]. Trichostatin A (TSA) is the inhibitors of the class I and class II HDACs with IC50 value of 2.4 ± 0.5 nM (measured by HDAC activity in cellular extracts). Trichostatin A treatment with concentration of 2 μM for 24h can increase histone H4 hyperacetylation in all of the breast cancer cell lines tested (MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3) significantly and inhibit the cell growth with IC50 values ranging in 26 – 308 nM in 96h. Treatment of 500 μg/kg trichostatin A by s.c injection daily for 4 weeks significantly inhibited tumor growth in Ludwig/Wistar/Olac female rats bearing tumors induced with NMU, compared with control[2]. Trichostatin A is usually used in the study of tumor growth inhibition. The cell death and cell cycle arrest induced by it may involve in several mechanisms including transcription-dependence and -independence, such as cell cycle arrest, apoptosis, the regulation of ROS and the inhibition of angiogenesis[3]. |
作用机制 | Trichostatin A comprises a hydroxamic acid-based metal-binding domain that coordinates the catalytic Zn(II) in the HDAC active site[4]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A2780 | 0.05-2 μM | Growth Inhibition Assay | 10/24/48 h | mediates growth arrest in a concentration- and time-dependent manner | 24223801 |
A431 | 2/10/50/100nM | Apoptosis Assay | 48h | inhibits the cell growth | 25371069 |
A431 | 50nM | Function Assay | 2/6/12/24h | activates p21 and inhibits ATF3 expression | 25371069 |
A549 | 1-10μM | Growth Inhibition Assay | 24h | IC50 of 3.2μM | 25169491 |
Dose | Mice[5] (i.p.): min = 0.5 mg/kg, max = 80 mg/kg | ||||||||||
Administration | i.p. | ||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03049124 | Rectal Cancer | Not Applicable | Recruiting | July 31, 2019 | Canada, Ontario ... 展开 >> University of Ottawa Recruiting Ottawa, Ontario, Canada, K1N 6N5 Contact: Amanda Wurz, MSc 613-562-5800 ext 3626 amanda.wurz@uottawa.ca 收起 << |
NCT02152267 | Craniomandibular Disorders | Not Applicable | Completed | - | Brazil ... 展开 >> Federal University of Bahia Salvador, Bahia, Brazil, 40110-902 收起 << |
NCT01028014 | Urethral Sphincter Activity | Not Applicable | Completed | - | United States, Alabama ... 展开 >> University of Alabama at Birmingham, The Kirklin Clinic Birmingham, Alabama, United States, 35233 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.31mL 0.66mL 0.33mL |
16.54mL 3.31mL 1.65mL |
33.07mL 6.61mL 3.31mL |
CAS号 | 58880-19-6 |
分子式 | C17H22N2O3 |
分子量 | 302.37 |
别名 | 曲古柳菌素A ;TSA |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 50 mg/mL(165.36 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 |
动物实验配方 |
2% DMSO+30% PEG 300+2% Tween 80+water 1.5 mg/mL |