2. Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Small Interfering RNA (siRNA) HDAC Apoptosis
  4. HDAC/PSMD14-IN-1

HDAC/PSMD14-IN-1 (Compound 8B) 是一种硫藤黄素衍生物。HDAC/PSMD14-IN-1 是一种具有口服活性的 PSMD14/HDAC1 双靶点抑制剂 (IC50 分别为 238.7 nM/141.2 nM)。HDAC/PSMD14-IN-1 对 ESCC 细胞系具有良好的细胞毒性 (IC50: 30-250 nM)，并有效逆转上皮间质转化 (EMT)。HDAC/PSMD14-IN-1 可诱导细胞凋亡 (Apoptosis)。HDAC/PSMD14-IN-1 在 KYSE30 细胞小鼠异种移植模型中具有抗肿瘤活性。HDAC/PSMD14-IN-1 可用于抗食管癌的研究。

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HDAC/PSMD14-IN-1 Chemical Structure

HDAC/PSMD14-IN-1 Chemical Structure

CAS No. : 3062141-62-9

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HDAC/PSMD14-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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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

HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research[1].

IC50 & Target[1]

HDAC1

141.2 nM (IC50)

药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1.6 mg/kg i.v. CL 7.3417 mL/min/kg
Mice 3 mg/kg p.o. AUC0-∞ 5.199 μg·h/mL
Mice 1.6 mg/kg i.v. T1/2 6.65 hr
Mice 3 mg/kg p.o. AUC0-t 5.138 μg·h/mL
Mice 1.6 mg/kg i.v. Cmax 3486.7 ng/mL
Mice 3 mg/kg p.o. T1/2 3.63 hr
Mice 1.6 mg/kg i.v. AUC0-∞ 3.6375 μg·h/mL
Mice 3 mg/kg p.o. Cmax 1085.0 ng/mL
Mice 1.6 mg/kg i.v. AUC0-t 3.5712 μg·h/mL
Mice 3 mg/kg p.o. Tmax 0.670 hr
Mice 1.6 mg/kg i.v. Tmax 0.0833 hr
分子量

432.56

Formula

C20H24N4O3S2
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/PSMD14-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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.

Keywords:

HDAC/PSMD14-IN-13062141-62-9Small Interfering RNA (siRNA)HDACApoptosisHistone deacetylasesAnti-esophageal cancerKYSE30 cell mouse xenograft modelKYSE 30KYSE 150KYSE 450ESCCThiolutinInhibitorinhibitorinhibit

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