2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC Histone Demethylase
  4. LSD1/HDAC-IN-3

LSD1/HDAC-IN-3 是一种靶向 class I HDAC 和 LSD1 的抑制剂。LSD1/HDAC-IN-3 抑制 HDAC1、HDAC2、HDAC3 和 LSD1，其 IC50 值分别为 1702 nM、842 nM、358 nM 和 1074 nM。LSD1/HDAC-IN-3 在 H2O2 处理的 ARPE-19 和 661W 视网膜细胞中表现出抗氧化作用，提高乙酰化和 组蛋白 H3 甲基化的水平。LSD1/HDAC-IN-3 在 rd10 视网膜色素变性小鼠模型中增强了光感受器的存活。LSD1/HDAC-IN-3 可用于研究如视网膜色素变性 (RP) 等遗传性视网膜疾病。

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LSD1/HDAC-IN-3

LSD1/HDAC-IN-3 Chemical Structure

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Customer Review

LSD1/HDAC-IN-3 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

查看 Histone Demethylase 亚型特异性产品:

查看所有亚型
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1/HDAC-IN-3 is a inhibitor targeting class I HDAC and LSD1 enzymes. LSD1/HDAC-IN-3 inhibits HDAC1, HDAC2, HDAC3, and LSD1 with IC50 values of 1702 nM, 842 nM, 358 nM, and 1074 nM, respectively. LSD1/HDAC-IN-3 exhibits antioxidant effects in H2O2-stressed ARPE-19 and 661W retinal cells, increasing levels of acetylated and methylated histone H3. LSD1/HDAC-IN-3 enhances photoreceptor survival in the rd10 mouse model of retinitis pigmentosa. LSD1/HDAC-IN-3 can be used for the study of inherited retinal diseases such as retinitis pigmentosa (RP)[1].

IC50 & Target[1]

HDAC1

1702 nM (IC50)

HDAC2

842 nM (IC50)

HDAC3

358 nM (IC50)

LSD1

1074 nM (IC50)

体外研究
(In Vitro)

LSD1/HDAC-IN-3 (Compound (±)-3d) 对 class I HDACs 和 LSD1 表现出抑制活性，其 IC50 值分别为 1702 nM (HDAC1)、842 nM (HDAC2)、358 nM (HDAC3) 和 1074 nM (LSD1)，而对 HDAC6、HDAC8 或 HDAC10 未表现出显著抑制作用[1]。
LSD1/HDAC-IN-3 (10-30 μM，24 h) 能显著保护 ARPE-19 和 661W 细胞免受 H2O2 诱导的氧化损伤，其证据为细胞存活率的提高[1]。
LSD1/HDAC-IN-3 (10 μM，24 h) 可在 ARPE-19 和 661W 细胞中部分提高乙酰化组蛋白 H3 (ac-H3) 和甲基化组蛋白 H3 (met-H3) 的水平[1]。

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

LSD1/HDAC-IN-3 相关抗体:
体内研究
(In Vivo)

LSD1/HDAC-IN-3 (Compound (±)-3d) (10 μM (1 μL/eye)，玻璃体腔注射，双侧单次给药) 可在具有 C57Bl/6J 背景的 Pde6b 纯合突变 rd10 小鼠的视网膜组织中增强光感受器的存活[1]。

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

Animal Model: Rd10 mice (autosomal recessive retinitis pigmentosa model with homozygous Pde6b mutation on C57Bl/6J background, both male and female, postnatal day 40)[1]
Dosage: 10 μM (1 μL/eye)
Administration: intravitreal injection, single bilateral administration
Result: Enhanced photoreceptor survival.
Preserved retinal pigment epithelium (RPE) barrier integrity, significantly increasing the number of Zonula Occludens-1 (ZO-1) positive intersections.
Downregulated retinal expression of inflammatory genes, specifically reducing the mRNA levels of GFAP, Ccl2, and Ccl12 in retinal tissues, and decreasing GFAP immunoreactivity.
Promoted histone H3 modifications in retinal tissues, inducing an upward trend in the levels of acetylated histone H3 (ac-H3) and methylated histone H3 (met-H3).
Showed no improvement in retinal function.
Exhibited good in vivo safety, with no signs of general distress or ocular tissue side effects.
分子量

440.58

Formula

C28H32N4O
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

LSD1/HDAC-IN-3 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:

LSD1/HDAC-IN-3HDACHistone DemethylaseHistone deacetylasesLSD1retinitis pigmentosaARPE-19661W retinal cellsInhibitorinhibitorinhibit

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