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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 | Citarinostat (ACY241) is an orally available, and highly selective inhibitor of HDAC6, showing an IC50 of 2.6 nM. Its selectivity extends across other HDAC isoforms as well, with IC50 values of 35 nM, 45 nM, 46 nM, and 137 nM for HDAC1, HDAC2, HDAC3, and HDAC8, respectively, suggesting its potential for anticancer applications[1]. |
| 体内研究 | Furthermore, in vivo studies reveal that Citarinostat, dosed at 50 mg/kg via intraperitoneal injection once daily for five days followed by a two-day break for three weeks, significantly inhibits tumor growth. This effect is observed in female athymic nude mice when Citarinostat is used in conjunction with NSC 125973, highlighting its therapeutic potential in cancer treatment when possibly combined with other anticancer agents. |
| 体外研究 | When administered to A2780 cells at a concentration of 300 nM for 24 hours, Citarinostat leads to notable hyperacetylation of α-tubulin, indicating the inhibition of HDAC6's tubulin deacetylase activity. Conversely, significant hyperacetylation of histone H3, a Class I HDAC target, is observed only at concentrations exceeding 1 μM. This delineates Citarinostat's capability for selective inhibition of HDAC6 at lower doses, while higher doses inhibit Class I HDAC isozymes[1]. In terms of cytotoxicity, Citarinostat's IC50 values span from 4.6 to 6.1 μM in A2780 and TOV-21G ovarian cancer cells, as well as in MDA-MB-231 breast cancer cells. The data indicate that lower doses of Citarinostat up to 3 μM modestly reduce cell proliferation without triggering apoptosis. However, a higher dose of 10 μM markedly induces apoptosis and entirely halts proliferation[1]. |
| Concentration | Treated Time | Description | References | |
| S1 cells | 2.82 ± 0.40 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on S1 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| MM.1s | 100-500 nM | 18 hours | To evaluate the selectivity of ACY-241 in MM cells. Results showed that ACY-241 selectively increased acetylation of α-Tubulin at low concentrations and increased acetylation of Histone-H3 at higher concentrations. | PLoS One. 2017 Mar 6;12(3):e0173507. |
| KP lung cancer cells | 10 µg/ml | 36 hours | To evaluate the effect of ACY241 and Oxaliplatin on the effector function of tumor-associated T cells, results showed that ACY241 or Oxaliplatin alone enhanced the ability of CD8+ T cells to secrete TNFα and IFNγ, and the combination treatment had a more pronounced effect. | Oncoimmunology. 2022 Feb 22;11(1):2042065. |
| CD4+ CD127loCD25+ Tregs | 500nM | 72 hours | To evaluate the impact of HDAC6-selective inhibitors on regulatory T-cells (Tregs). Results showed that ACY-241 reduced Treg frequencies and FOXP3 expression and decreased their suppressive function. | J Immunother Cancer. 2019 Feb 6;7(1):33. |
| R482-HEK293 cells | 20.11 ± 2.48 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on R482-HEK293 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| MDR19-HEK293 cells | 33.83 ± 3.21 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on MDR19-HEK293 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| HEK293 cells | 3.01 ± 0.44 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on HEK293 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| S1-M1-80 cells | 59.66 ± 10.32 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on S1-M1-80 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| KB-V-1 cells | 57.96 ± 5.56 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on KB-V-1 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| KB-3-1 cells | 3.98 ± 0.73 µM | 72 hours | Evaluate the cytotoxicity of Citarinostat on KB-3-1 cells | Int J Mol Sci. 2021 Mar 5;22(5):2592. |
| T-cells from melanoma patient PBMCs | 500nM | 72 hours | To evaluate the impact of HDAC6-selective inhibitors on T-cell viability and function. Results showed that ACY-241 did not impair T-cell viability at concentrations up to 1uM and reduced Th2 cytokine production (i.e. IL-4, IL-5, IL-6, IL-10 and IL-13). | J Immunother Cancer. 2019 Feb 6;7(1):33. |
| Granta-519 | 0, 0.5, 1, 2, 4 µM | 24-48 hours | To evaluate the cytotoxicity of Citarinostat and Momelotinib alone and in combination on Granta-519 cells. Results showed that Granta-519 cells were less sensitive to the combination treatment (CI > 1), exhibiting an antagonistic effect. | Apoptosis. 2020 Jun;25(5-6):370-387. |
| WSU-NHL | 0, 0.5, 1, 2, 4 µM | 24-48 hours | To evaluate the cytotoxicity of Citarinostat and Momelotinib alone and in combination on lymphoid malignant cell lines. Results showed that the combination of Citarinostat and Momelotinib exhibited synergistic effects (CI < 1) in most cell lines, significantly inhibiting cell viability and inducing apoptosis. | Apoptosis. 2020 Jun;25(5-6):370-387. |
| Administration | Dosage | Frequency | Description | References | ||
| CB.17 SCID mice | H929 MM xenograft model | Intraperitoneal injection | 50 mg/kg (ACY-241), 1 mg/kg (pomalidomide) | Once daily for 42 consecutive days | To evaluate the effect of combination treatment with ACY-241 and pomalidomide on tumor growth in the H929 MM xenograft model. Results showed that combination treatment significantly inhibited tumor growth without significant toxicity or adverse effects. | PLoS One. 2017 Mar 6;12(3):e0173507. |
| Mice | KP lung cancer model | Intraperitoneal injection | 25 mg/kg (ACY241), 10 mg/kg (Oxaliplatin) | ACY241 3 times/week for 3 weeks; Oxaliplatin 1 time/week for 6 weeks | To evaluate the therapeutic effect of ACY241 alone or in combination with Oxaliplatin, results showed that combination therapy significantly prolonged the survival of mice and enhanced the effector function of tumor-associated T cells. | Oncoimmunology. 2022 Feb 22;11(1):2042065. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.14mL 0.43mL 0.21mL |
10.68mL 2.14mL 1.07mL |
21.37mL 4.27mL 2.14mL |
|
| CAS号 | 1316215-12-9 |
| 分子式 | C24H26ClN5O3 |
| 分子量 | 467.95 |
| SMILES Code | O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O |
| MDL No. | MFCD28023593 |
| 别名 | ACY241; HDAC-IN-2 |
| 运输 | 蓝冰 |
| InChI Key | VLIUIBXPEDFJRF-UHFFFAOYSA-N |
| Pubchem ID | 53340426 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 30 mg/mL(64.11 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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