1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. HDAC6-IN-44

HDAC6-IN-44 (compound H10) 是一种选择性 HDAC6 抑制剂,IC50 值为 8.97 nM,HDAC6-IN-44 能够抑制特发性肺纤化维表型,具有抗肺纤维化活性。HDAC6-IN-44 在博来霉素诱导的肺纤维化小鼠模型中被验证可抑制肺纤维化进程,且具有良好的代谢稳定性,HDAC6-IN-44 有望用于特发性肺纤化领域研究。

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HDAC6-IN-44 Chemical Structure

HDAC6-IN-44 Chemical Structure

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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-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis[1].

IC50 & Target[1]

HDAC6

8.97 nM (IC50)

HDAC1

878 nM (IC50)

HDAC2

3144 nM (IC50)

HDAC4

847 nM (IC50)

HDAC7

894 nM (IC50)

HDAC10

1319 nM (IC50)

HDAC11

>5000 nM (IC50)

体外研究
(In Vitro)

HDAC6-IN-44 (compound H10) (2.5-10 μM, 1-300 μM, 48 h) 以剂量依赖的方式抑制 TGF-β 诱导的 HELF 细胞增殖、细胞活力及其 HDAC6 活性,且未引起明显的细胞毒性效应[1]
HDAC6-IN-44 (2.5-10 μM, 48h) 通过作用于 HDAC6 相关信号通路干预 TGF-β1 相关的纤维化过程[1]

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

Cell Viability Assay[1]

Cell Line: HELF cells
Concentration: 2.5-10 μM (cell proliferation test), 1-300 μM (survival toxicity test)
Incubation Time: 48 h
Result: Inhibited TGF-β-induced HELF cell proliferation without significantly inhibiting cell survival at a maximum concentration of approximately 10 μM.

Western Blot Analysis[1]

Cell Line: HELF cells
Concentration: 2.5-10 μM
Incubation Time: 48 h
Result: Exhibited dose-dependent increase in acetylated α-tubulin expression and has no effect on histone H3 acetylation, while attenuating the elevated expression of all marker proteins induced by TGF-β1.
体内研究
(In Vivo)

HDAC6-IN-44 (compound H10) (0.1 mL/10g, 腹腔注射, 每日注射持续三周) 对肺纤维化小鼠模型中肺组织 HDAC6 活性增加及胶原沉积具有显著抑制作用[1]
HDAC6-IN-44 (0.1 mL/10g, 腹腔注射, 每日注射持续三周) 能够剂量依赖性地抑制肺纤维化小鼠模型的肺纤维化的进程[1]

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

Animal Model: Bleomycin-induced pulmonary fibrosis mouse model[1]
Dosage: 0.1 mL/10g
Administration: Intraperitoneal injection (i.p.) , daily for 3 weeks
Result: Caused the blue collagen fiber deposition to be spot-like, with the surrounding alveolar cavity slightly collapsed and the alveolar wall thickened, but the collagen fiber deposition was significantly less than that in the model group. Additionally, HDAC6-IN-44 could dose-dependently inhibit the expression of α-SMA and p-Smad2/3 in BLM-induced pulmonary fibrosis in mice.
分子量

351.40

Formula

C20H21N3O3

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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-44
目录号:
HY-162630
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