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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-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 (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 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 | 
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| 描述 | Histone deacetylases (HDACs) participate in the control of cellular biological processes via specificly removing acetyl groups on lysine residues in histones and non-histone proteins. The isoform of HDAC6 is orientated in the cytoplasm and mainly interacts with non-histone proteins. It plays a central role in microtubule-dependent cell motility via deacetylation of tubulin. In addition to its protein deacetylase activity, HDAC6 plays a key role in the degradation of misfolded proteins. Nexturastat A is a HDAC6 selective inhibitor with IC50 of 5.02nM, while the IC50s of it against HDAC1, 2, 3, 4, 5, 7, 8, 9, 10, 11 were 3.02μM, 6.92μM, 6.68μM, 9.39μM, 11.7μM, 4.46μM, 0.95μM, 6.72μM, 7.57μM and 5.14μM, respectively[3]. Treatment of B16 cells with Nexturastat A at doses ranging from 1nM to 10000nM concentration dependently increased acetyl-tubulin levels[3]. 10μM, 20μM , 30μM and 40μM Nexturastat A dose-dependently impaired the viability of multiple myeloma PRMI-8226 and U266 cell lines. 48h treatment of Nexturastat A at the concentration of 40μM induced apoptosis in RPMI-8226 and U266 cells[4]. In SM1 murine melanoma tumor model established in C57BL/6 mice, Nexturastat A was administrated 5 times a week at the dose of 15mg/kg, or in combination of anti-PD-1 for 25 days. At day25, the tumor volume of the combination group, Nexturastat A group, anti-PD-1 group and control group were 257.3mm3, 750.1 mm3, 1030 mm3 and 2034 mm3, respectively[5]. | 
| Concentration | Treated Time | Description | References | |
| WM164 human melanoma cells | 5 µM | 24 hours | HDAC6 knockdown downregulated CD47 expression and prevented IFNγ-driven CD47 upregulation. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| B16 melanoma cells | 5 µM | 24 hours | Nexturastat A repressed IFNγ-driven Cd47 upregulation. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| SM1 melanoma cells | 5 µM | 24 hours | Nexturastat A repressed IFNγ-driven Cd47 upregulation. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| THP-1-derived macrophages | 5 µM | 24 hours | Nexturastat A significantly upregulated M1-associated markers NOS2, CD86, and IL1B and downregulated M2-associated markers MRC1 and CD209. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| A31A7 macrophages | 5 µM | 24 hours | Nexturastat A significantly upregulated surface expression of M1-associated markers Cd80 and H2 and downregulated surface expression of M2-associated marker Cd206. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| Bone marrow-derived macrophages (BMDMs) | 5 µM | 24 hours | Nexturastat A significantly upregulated M1-associated markers Nos2 and Cd80 and downregulated M2-associated markers Arg1 and Mrc1 at the transcriptional level. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| Mouse peritoneal elicited macrophage (PEM) | 5 µM | 24 hours | To evaluate the effect of Nexturastat A on macrophage polarization, results showed that NextA reduced the expression of M2 marker CD206 and increased the M1 phenotype. | Sci Rep. 2019 Apr 16;9(1):6136. | 
| SM1 melanoma cells | 2.5 and 5 µM | 24 hours | To evaluate the effect of Nexturastat A on PD-L1 expression, results showed that NextA neutralized the anti-PD1 antibody-mediated upregulation of IFNγ on PD-L1 production. | Sci Rep. 2019 Apr 16;9(1):6136. | 
| RPMI-8226/BTZ100 cells | 20 µM | 48 hours | To evaluate the effect of NexA on BTZ-resistant cell viability, results showed that NexA remarkably suppressed the viability of RPMI-8226/BTZ100 cells. | Biosci Rep. 2019 Mar 22;39(3):BSR20181916. | 
| U266 cells | 30 µM | 48 hours | To evaluate the effect of NexA on cell viability, results showed that NexA dose-dependently impaired the viability of the two cell lines. | Biosci Rep. 2019 Mar 22;39(3):BSR20181916. | 
| RPMI-8226 cells | 30 µM | 48 hours | To evaluate the effect of NexA on cell viability, results showed that NexA dose-dependently impaired the viability of the two cell lines. | Biosci Rep. 2019 Mar 22;39(3):BSR20181916. | 
| OVSAHO | 12500 nM | 48 hours preincubation followed by 72 hours incubation | Nexturastat A increased cisplatin potency in OVSAHO cells, with IC50 values in the micromolar range. | Int J Mol Sci. 2019 Jun 22;20(12):3052. | 
| Kuramochi | 5000 nM | 48 hours preincubation followed by 72 hours incubation | Nexturastat A increased cisplatin potency in Kuramochi cells, with IC50 values in the micromolar range. | Int J Mol Sci. 2019 Jun 22;20(12):3052. | 
| HEY | 5000 nM | 48 hours preincubation followed by 72 hours incubation | Nexturastat A increased cisplatin potency in HEY cells, with IC50 values in the micromolar range. | Int J Mol Sci. 2019 Jun 22;20(12):3052. | 
| CaOV3 | 7500 nM | 48 hours preincubation followed by 72 hours incubation | Nexturastat A increased cisplatin potency in CaOV3 cells, with IC50 values in the micromolar range. | Int J Mol Sci. 2019 Jun 22;20(12):3052. | 
| A2780 | 7500 nM | 48 hours preincubation followed by 72 hours incubation | Nexturastat A increased cisplatin potency in A2780 cells, with IC50 values in the micromolar range. | Int J Mol Sci. 2019 Jun 22;20(12):3052. | 
| HeLa cells | 2.5 µM | 72 hours | Nexturastat A increased BE3-mediated gene editing efficiency in HeLa cells, with an average improvement of 4.90-fold. | Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986. | 
| HT1080 cells | 2.5 µM | 72 hours | Nexturastat A significantly improved BE3-mediated gene editing efficiency in HT1080 cells, with an average improvement of 7.96-fold. | Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986. | 
| HEK-293 cells | 2.5 µM | 72 hours | Nexturastat A increased BE3-mediated gene editing efficiency, with an average improvement of 3.46-fold. | Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986. | 
| BT474 | 0.37 nM to 100 µM | 72 hours | Evaluate the cytotoxic effect of Nexturastat A on HER2+ breast cancer cells, showing that NextA was effective in both SKBR3 and BT474 cell lines. | Cancers (Basel). 2024 Nov 6;16(22):3752. | 
| SKBR3 | 0.37 nM to 100 µM | 72 hours | Evaluate the cytotoxic effect of Nexturastat A on HER2+ breast cancer cells, showing that NextA was effective in both SKBR3 and BT474 cell lines, with the lowest IC50 in SKBR3 clones. | Cancers (Basel). 2024 Nov 6;16(22):3752. | 
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Oct4-eGFP mice | Added to embryo culture medium | 0.5 µM | 24 hours | Nexturastat A significantly improved BE3-mediated gene editing efficiency, with a 1.57-fold improvement in embryos. | Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986. | 
| C57BL/6 mice | SM1 melanoma model | Subcutaneous injection | 15 mg/kg | 5 days a week for 25 days | To evaluate the effect of Nexturastat A in combination with anti-PD-1 antibody, results showed that the combination significantly reduced tumor growth and enhanced immune cell infiltration. | Sci Rep. 2019 Apr 16;9(1):6136. | 
| C57BL/6 mice | SM1 melanoma model | Intraperitoneally | 20 mg/kg | Every other day until the end of the study | The combination of Nexturastat A and anti-CD47 significantly decreased tumor growth, increased immune cell infiltration in the tumor microenvironment (TME), and modulated macrophage and natural killer (NK) cell populations. | J Exp Clin Cancer Res. 2024 Feb 27;43(1):60. | 
| Mice | Listeria infection model | Intraperitoneal injection | 3 mg/kg | 5 days post infection | Reduced Listeria burdens, increased Th1 cell numbers | Cell Death Differ. 2022 Nov;29(11):2303-2315 | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 2.93mL 0.59mL 0.29mL | 14.65mL 2.93mL 1.46mL | 29.29mL 5.86mL 2.93mL | |
| CAS号 | 1403783-31-2 | 
| 分子式 | C19H23N3O3 | 
| 分子量 | 341.4 | 
| SMILES Code | O=C(NO)C1=CC=C(CN(CCCC)C(NC2=CC=CC=C2)=O)C=C1 | 
| MDL No. | MFCD28099804 | 
| 别名 | |
| 运输 | 蓝冰 | 
| InChI Key | JZWXMCPARMXZQV-UHFFFAOYSA-N | 
| Pubchem ID | 71462653 | 
| 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: 55 mg/mL(161.1 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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			沪ICP备2024050318号-1