2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-45

HDAC-IN -45 (Compound 14) 是一种小分子 HDAC 抑制剂，具有抗癌活性，也可与 Y303 残基形成氢键。HDAC-IN-45 (Compound 14) 对 HDAC1、2 和 3 亚型具有显著的抑制作用， IC50 分别为 0.108、0.585 和 0.563 μM。

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HDAC-IN-45 Chemical Structure

HDAC-IN-45 Chemical Structure

CAS No. : 2421122-61-2

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HDAC-IN-45 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively[1].

IC50 & Target[1]

HDAC1

0.108 μM (IC50)

HDAC2

0.585 μM (IC50)

HDAC3

0.563 μM μM (IC50)

HDAC6

﹥10 μM (IC50)

HDAC8

6.81 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 IC50
2.44 μM
Compound: 14
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32325365]
MDA-MB-231 IC50
1.48 μM
Compound: 14
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32325365]
体外研究
(In Vitro)

HDAC-IN-45 (Compound 14) suppresses the growth of triple-negative breast cancer cells MDA-MB-231 (IC50 = 1.48 μM), MDA-MB-468 (IC50= 0.65 μM), and liver cancer cells HepG2 (IC50= 2.44 μM).
HDAC-IN-45 has equally virulent in the HDAC-sensitive cell lines (YCC11) and -resistant gastric cell lines (YCC3/7) and overcome HDACi resistance. HDAC-IN-45 has a high toxicity (IC50= 0.33 μM) in three leukemic cell lines, K-562, KG-1 and THP-1.
HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
HDAC-IN-45 (Compound 14) can elevate acetylation level of histone H3 and expression of p21.
HDAC-IN-45 (Compound 14) exerts a dose-dependent upregulation of ac-H3K9 in MDA-MB-231 cells, triggers cell cycle arrest in G1 phase.
HDAC-IN-45 (Compound 14) exhibits a potent antitumor efficacy in xenograft mouse model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC-IN-45 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Triple-negative breast cancer cells; liver cancer cells; YCC11 and YCC3/7
Concentration: a series of concentration
Incubation Time: 72 h
Result: Inhibited the cell growth viability of HepG2 and triple-negative breast cancer cells.

Cell Cytotoxicity Assay[1]

Cell Line: Three leukemic cell lines (K-562, KG-1 and THP-1); YCC3/7 and YCC11 cell lines
Concentration: a series of concentration
Incubation Time: 72 h
Result: Showed a potent anti-cancer effect, exhibited high sensitivities and strong toxicities with IC50 values below micromolar in leukemic cell lines.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2 µM
Incubation Time: 24 h
Result: Elevated acetylation level of histone H3 and expression of p21.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231cells
Concentration: 4 µM
Incubation Time: 24 h
Result: Arrested cell cycle in G1 and trigger apoptosis.
体内研究
(In Vivo)

HDAC-IN-45 (Compound 14) (25 mg/kg or 50mg/kg; i.p.; every day) exhibits a potent antitumor efficacy in human MDA-MB-231 breast cancer xenograft mouse model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human MDA-MB-231 breast cancer xenograft mouse model[1]
Dosage: 25 mg/kg or 50mg/kg
Administration: 25 mg/kg or 50mg/kg; i.p.; every day.
Result: Exhibited a potent antitumor efficacy.
分子量

502.93

Formula

C25H20ClFN8O
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

HDAC-IN-45 相关分类

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  • 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.

Keywords:

HDAC-IN-452421122-61-2HDACHistone deacetylasesHDAC inhibitortumorcancerInhibitorinhibitorinhibit

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