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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-B, IC50: 7.5 nM HD1-A, IC50: 16 nM |
+++
HD2, IC50: 10 nM |
99%+ | ||||||||||||||||
| MC1568 |
++
HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM |
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 |
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 | ✔ | NF-κB,p53 | 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 | PCI-34051 is an inhibitor of pure recombinant HDAC8, exhibits a Ki of 10 nM, demonstrating >200-fold selectivity over other tested HDACs, including HDACs 1, 2, 3, 6, and 10. Derived from a low molecular weight hydroxamic acid scaffold, PCI-34051 initially possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to other class I HDACs. In cell lines derived from T-cell lymphomas, such as Jurkat and HuT78, PCI-34051 induces apoptosis at low micromolar concentrations, while doses as high as 20 μM have no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines [1]. |
| 体内研究 | The administration of PCI-34051 and dexamethasone effectively reduces eosinophilic inflammation and airway hyperresponsiveness in asthma, thereby mitigating airway remodeling [2]. |
| 体外研究 | PCI-34051 is an inhibitor of pure recombinant HDAC8, exhibits a Ki of 10 nM, demonstrating >200-fold selectivity over other tested HDACs, including HDACs 1, 2, 3, 6, and 10. Derived from a low molecular weight hydroxamic acid scaffold, PCI-34051 initially possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to other class I HDACs. In cell lines derived from T-cell lymphomas, such as Jurkat and HuT78, PCI-34051 induces apoptosis at low micromolar concentrations, while doses as high as 20 μM have no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines [1]. |
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| human Huh7 cells | Function assay | 3 days | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50=1.8 μM | 25490700 | |
| human Jurkat cells | Growth inhibition assay | 72 h | Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay, GI50=11 μM | 23116147 | |
| human MT2 cells | Growth inhibition assay | 72 h | Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay, GI50=15 μM | 23116147 | |
| human MT4 cells | Growth inhibition assay | 72 h | Growth inhibition of human MT4 cells incubated for 72 hrs by MTS assay, GI50=25 μM | 23116147 | |
| Dose | Mice(i.p.): 0.5 mg/kg[3], 3 mg/kg[4] |
| Administration | i.p. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.37mL 0.67mL 0.34mL |
16.87mL 3.37mL 1.69mL |
33.75mL 6.75mL 3.37mL |
|
| CAS号 | 950762-95-5 |
| 分子式 | C17H16N2O3 |
| 分子量 | 296.32 |
| SMILES Code | O=C(C1=CC2=C(C=C1)C=CN2CC3=CC=C(OC)C=C3)NO |
| MDL No. | MFCD11114393 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | AJRGHIGYPXNABY-UHFFFAOYSA-N |
| Pubchem ID | 24753719 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 30 mg/mL(101.24 mM),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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