1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. 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。

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HDAC6-IN-4 Chemical Structure

HDAC6-IN-4 Chemical Structure

CAS No. : 2709103-20-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

IC50 & Target

HDAC6

23 nM (IC50)

HDAC3

46 nM (IC50)

HDAC2

172 nM (IC50)

HDAC8

2175 nM (IC50)

HDAC1

3604 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
5.77 μM
Compound: C10
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 35245830]
B16 IC50
1.52 μM
Compound: C10
Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay
Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay
[PMID: 35245830]
CT26 IC50
2.09 μM
Compound: C10
Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay
Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay
[PMID: 35245830]
HepG2 IC50
2.36 μM
Compound: C10
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 35245830]
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].

MCE 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.
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].

MCE 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.
分子量

506.63

Formula

C30H38N2O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HDAC6-IN-4
目录号:
HY-144395
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