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HDAC6-IN-4
HDAC6-IN-4 (C10) 是一种有效的、具有口服活性的、高选择性的 HDAC6 抑制剂， IC50 值为23 nM。HDAC6-IN-4 诱导肿瘤细胞凋亡 (apoptosis)，具有显著的抗肿瘤作用，且无明显毒性。
HDAC6-IN-4 Chemical Structure
CAS No. : 2709103-20-6
| 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 |
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1].
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| IC50 & Target |
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HDAC6
23 nM (IC50)
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HDAC3
46 nM (IC50)
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HDAC2
172 nM (IC50)
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HDAC8
2175 nM (IC50)
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HDAC1
3604 nM (IC50)
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体外研究
(In Vitro) |
HDAC6-IN-4 (C10) (0-50 µM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity[1].
HDAC6-IN-4 (0-6 µM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1[1].
HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells[1].
HDAC6-IN-4 (0-8 µM, 24 h) induces B16 cell apoptosis in a dose-dependent manner[1].
HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
| Cell Line: |
B16, HepG2, A549, and CT26 cells |
| Concentration: |
0-50 µM |
| Incubation Time: |
72 h |
| Result: |
Showed antiproliferative activity with IC50 values of 1.52, 2.36, 5.77, and 2.09 µM against B16, HepG2, A549, and CT26 cells, respectively. |
Western Blot Analysis[1]
| Cell Line: |
B16 and CT26 cancer cells |
| Concentration: |
2, 4, and 6 µM |
| Incubation Time: |
2, 4, 8, 12, and 24 h |
| Result: |
Dramatically increased the level of Ac-Tub (acetyl-α-tubulin) in a dose-dependent and time-dependent manner. Had almost no effect on the content of Ac-H3 (acetyl-H3). |
Apoptosis Analysis[1]
| Cell Line: |
B16 cells |
| Concentration: |
4, 6, and 8 µM |
| Incubation Time: |
24 h |
| Result: |
Caused moderate to potent induction of apoptosis in the B16 cell line in a dose-dependent manner. Upregulated the expression of apoptotic protein cleaved PARP. |
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体内研究
(In Vivo) |
HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Five-week-old C57BL/6 mice (immune-related CT26 xenograft model)[1]. |
| Dosage: |
50 and 100 mg/kg |
| Administration: |
Oral gavage, once daily for 21 days |
| Result: |
Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity. |
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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]. Xi Xu, et al. Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. Eur J Med Chem. 2022 Apr 5;233:114228.
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