上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
HDAC-IN-36
HDAC-IN-36 (compound 23 g) 是一种口服有效的HDAC (组蛋白去乙酰化酶)抑制剂，其 IC50 为 11.68 nM (HDAC6)。HDAC-IN-36 可促进细胞凋亡 (apoptosis)，自噬 (autophagy) 和抑制迁移。HDAC-IN-36 具有抗肿瘤和抗转移活性，可用于乳腺癌研究。
HDAC-IN-36 Chemical Structure
CAS No. : 2482992-54-9
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].
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| IC50 & Target |
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HDAC6
11.68 nM (IC50)
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HDAC10
13.24 nM (IC50)
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HDAC3
79.17 nM (IC50)
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HDAC1
86.93 nM (IC50)
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HDAC2
97.32 nM (IC50)
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HDAC8
378.2 nM (IC50)
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HDAC4
>1000 nM (IC50)
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HDAC5
>1000 nM (IC50)
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HDAC7
>1000 nM (IC50)
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HDAC9
>1000 nM (IC50)
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HDAC11
>1000 nM (IC50)
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体外研究
(In Vitro) |
HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90[1].
HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis[1].
HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously[1].
HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
| Cell Line: |
MDA-MB-231 cells[1] |
| Concentration: |
0, 2.5, 5, 10 μM |
| Incubation Time: |
24 h |
| Result: |
Exhibited good anti-proliferative activity in MDA-MB-231 cells, with IC50 of 1.32 ± 0.13 μM, increased the acetylation level of intracellular proteins, and promoted the acetylation of α-Tubulin and HSP90. |
Apoptosis Analysis
| Cell Line: |
MDA-MB-231 cells[1] |
| Concentration: |
0, 2.5, 5, 10 μM |
| Incubation Time: |
24 h |
| Result: |
Induced apoptosis in MDA-MB-231 cells in a dose-dependent manner. |
Cell Autophagy Assay
| Cell Line: |
MDA-MB-231 cells[1] |
| Concentration: |
0, 2.5, 5, 10 μM |
| Incubation Time: |
24 h |
| Result: |
Induced noteworthy autophagy with increased aggregation of LC3 puncta. |
Western Blot Analysis
| Cell Line: |
MDA-MB-231 cells[1] |
| Concentration: |
0, 2.5, 5, 10 μM |
| Incubation Time: |
24 h |
| Result: |
Mainly induced mitochondrial-dependent apoptosis, up-regulated the expression of Bax and downregulated the expression of Bcl-2, and increased the cleavage of caspase3, caspase8 and caspase9; increased the expression of E-cadherin and decreased the expression of MMP-2 obviously; increased the expression of Beclin1, LC3II and decreased the expression of SQSTM1/p62. |
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体内研究
(In Vivo) |
HDAC-IN-36 (compound 23 g) (Zebrafish tumor xenograft model; 0-5 μg/mL, 3 days) shows potent anti-tumor and anti-metastatic activity, and improves in vivo anti-tumor efficacy[1].
HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters[1].
Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles[1].
| Parameters |
23g (20 mg/kg) |
| T1/2 (h) |
1.24 ± 0.21 |
| Tmax (h) |
0.79 ± 0.33 |
| Cmax (μg/L) |
120.36 ± 15.53 |
| AUC0-t (μg/L∗h) |
1275.35 ± 70.17 |
| AUC0-∞ (μg/L∗h) |
1289.40 ± 88.91 |
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)[1] |
| Dosage: |
0, 2.5, 5 μg/mL |
| Administration: |
3 days |
| Result: |
Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy. |
| Animal Model: |
Beagles (female, 8-10 kg, n = 4)[1] |
| Dosage: |
20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution) |
| Administration: |
Orally, once (Pharmacokinetic Analysis) |
| Result: |
Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Yao D, Li C, Jiang J, et al. Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer. Eur J Med Chem. 2020;205:112648.
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