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)

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

  • 摩尔计算器

  • 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.

Keywords:

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

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