2. Cell Cycle/DNA Damage Epigenetics Membrane Transporter/Ion Channel
  3. HDAC P-glycoprotein
  4. 2-Propylpent-4-ynoic acid

2-Propylpent-4-ynoic acid (4-yn-VPA) 是一种 HDAC 抑制剂 (对人源 HDAC 的 IC50=0.5 mM)。2-Propylpent-4-ynoic acid 还诱导 P-糖蛋白功能，还表现出致畸性、胎儿生长抑制及神经毒性。2-Propylpent-4-ynoic acid 具有显著的立体特异性致畸效应，其中 S-对映体的致畸性强于 R-对映体及其他类似物。2-Propylpent-4-ynoic acid 的神经毒性与立体化学结构无关。2-Propylpent-4-ynoic acid 已被应用于结肠癌发病机制及露脑畸形等神经管缺陷的相关研究中。

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2-Propylpent-4-ynoic acid

2-Propylpent-4-ynoic acid Chemical Structure

CAS No. : 24102-11-2

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2-Propylpent-4-ynoic acid 相关抗体

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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

2-Propylpent-4-ynoic acid (4-yn-VPA) is a HDAC inhibitor (with an IC50 of 0.5 mM against human HDAC). 2-Propylpent-4-ynoic acid also induces P-glycoprotein function, and exhibits teratogenicity, fetal growth inhibition and neurotoxicity. 2-Propylpent-4-ynoic acid shows significant stereospecific teratogenic effects, with the S-enantiomer being more teratogenic than the R-enantiomer and other analogs. The neurotoxicity of 2-Propylpent-4-ynoic acid is independent of its stereochemical structure. 2-Propylpent-4-ynoic acid has been used in studies related to the pathogenesis of colon cancer and neural tube defects such as exencephaly[1][2].

体外研究
(In Vitro)

2-Propylpent-4-ynoic acid (4-yn-VPA) (1 mM; 5 d) 可诱导人结肠腺癌 SW620 细胞中 P-gp 的功能，其在 HeLa 细胞核提取物中的 HDAC 抑制 IC50 为 0.5 mM[1]。

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

2-Propylpent-4-ynoic acid 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: human colon adenocarcinoma SW620 cells
Concentration: 1 mM
Incubation Time: 5 days
Result: Induced P-gp function with IC50 of 0.5 mM.
体内研究
(In Vivo)

2-Propylpent-4-ynoic acid (4-yn-VPA) 诱导小鼠出现露脑畸形时，S-(-)-4-yn-VPA 异构体 (0.40-1.05 mmol/kg；腹腔注射；妊娠第 8 天；单次) 的效力是 R(+)-4-yn-VPA 异构体的 7.5 倍 (3-6 mmol/kg；腹腔注射；妊娠第 8 天；单次) 的 7.5 倍，两者的 ED50 分别为 0.83 mmol/kg 和 6.19 mmol/kg[2]。

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

Animal Model: Han:NMRI (female, 29-36 g, neural tube defect induced by treatment on gestational day 8)[2]
Dosage: 0.40, 0.60, 0.73, 0.86, 1.05 mmol/kg (S(-)-4-yn-VPA);
3.00, 4.50, 6.00 mmol/kg (R(+)-4-yn-VPA)
Administration: i.p.; single dose on gestational day 8
Result: Induced exencephaly at rates of 3%, 23%, 38%, 51%, 65% for S(-)-4-yn-VPA at 0.40, 0.60, 0.73, 0.86, 1.05 mmol/kg, respectively.
Caused embryolethality at rates of 10%, 8%, 17%, 38%, 51% for S(-)-4-yn-VPA at 0.40, 0.60, 0.73, 0.86, 1.05 mmol/kg, respectively.
Reduced fetal weights significantly (vs control) to 1.05 g and 1.04 g for S(-)-4-yn-VPA at 0.86 mmol/kg and 1.05 mmol/kg, respectively.
Induced exencephaly at rates of 1%, 26%, 38% for R(+)-4-yn-VPA at 3.00, 4.50, 6.00 mmol/kg, respectively.
Caused embryolethality at rates of 10%, 16%, 45% for R(+)-4-yn-VPA at 3.00, 4.50, 6.00 mmol/kg, respectively.
Reduced fetal weight significantly (vs control) to 1.00 g ± 0.10 for R(+)-4-yn-VPA at 6.00 mmol/kg.
Achieved an ED50 of 0.83 mmol/kg for exencephaly induction with S(-)-4-yn-VPA, and 6.19 mmol/kg for R(+)-4-yn-VPA.
分子量

140.18

Formula

C8H12O2
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

2-Propylpent-4-ynoic acid 相关分类

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Keywords:

2-Propylpent-4-ynoic acid24102-11-24-yn-VPAHDACP-glycoproteinHistone deacetylasesP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243histone deacetylasecolon carcinomaHeLa nuclear extractsexencephalymicehuman colon adenocarcinoma SW620 cellsInhibitorinhibitorinhibit

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