2. JAK/STAT Signaling Apoptosis Autophagy
  3. Pim Apoptosis Autophagy
  4. Pim-1 kinase inhibitor 8

Pim-1 kinase inhibitor 8 

目录号: HY-162006 纯度: 99.90%
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Pim-1 kinase inhibitor 8 是一种强效的 PIM-1 抑制剂，IC50 值为 14.3 nM。Pim-1 kinase inhibitor 8 通过抑制 PIM-1 并诱导细胞凋亡 (apoptosis) 和自噬 (autophagy) 来抑制细胞的增殖与迁移。Pim-1 kinase inhibitor 8 能有效抑制实体艾氏腹水癌 (SEC) 荷瘤小鼠模型的肿瘤生长。Pim-1 kinase inhibitor 8 可用于乳腺癌和肝癌的相关研究。

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Pim-1 kinase inhibitor 8

Pim-1 kinase inhibitor 8 Chemical Structure

CAS No. : 916038-47-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1870
In-stock
5 mg ￥1700
In-stock
10 mg ￥2700
In-stock
25 mg ￥5400
In-stock
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Pim-1 kinase inhibitor 8 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pim-1 kinase inhibitor 8 is a potent PIM-1 inhibitor with an IC50 value of 14.3 nM. Pim-1 kinase inhibitor 8 impedes cell proliferation and migration through PIM-1 inhibition and the induction of both apoptosis and autophagy. Pim-1 kinase inhibitor 8 inhibits solid tumor growth in Solid Ehrlich Carcinoma (SEC)-bearing mice. Pim-1 kinase inhibitor 8 can be used for breast and liver cancer research[1].

体外研究
(In Vitro)

Pim-1 kinase inhibitor 8 (compound 12) (0.01-100 μM，48 小时) 对 MCF-7 和 HepG2 细胞系表现出强效细胞毒性，IC50 值分别为 0.51 μM 和 5.27 μM，而在正常 MCF-10A 细胞中表现出较低的细胞毒性 (IC50 = 52.85 μM)[1]。
Pim-1 kinase inhibitor 8 (1.62 μM，48 小时) 在 MCF-7 细胞中触发显著的凋亡与自噬性细胞死亡，伴有 S 期细胞周期阻滞，并且能显著抑制细胞迁移 (伤口愈合率为 71.8 %，而对照组为 95.6 %)[1]。
Pim-1 kinase inhibitor 8 通过与 Lys67 形成关键氢键和多重疏水相互作用与 PIM-1 活性位点紧密结合 (结合能为 -17.38 kcal/mol)[1]。

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

Pim-1 kinase inhibitor 8 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.62 μM
Incubation Time: 48 h
Result: Increased the proportion of cells in the S-phase to 36.02 %, compared to 29.12 % in the control.
Reduced the proportion of cells in the G2/M phase from 16.05 % (control) to 7.56 %.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.62 μM
Incubation Time: 48 h
Result: Increased total apoptosis by 33.43 % (23.18 % for early apoptosis and 10.25 % for late apoptosis) compared to the untreated control group (0.64 %).
Increased apoptosis by 52.2-fold.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 and HepG2 cells
Concentration: 0.01, 0.1, 1, 10, and 100 μM
Incubation Time: 48 h
Result: Inhibited the growth of MCF-7 and HepG2 cells by 84.20 % and 85.13 %, respectively, at 100 μM.

Cell Autophagy Assay[1]

Cell Line: MCF-7 cells
Concentration: 1.62 μM
Incubation Time: 48 h
Result: Caused considerable autophagic cell death, markedly increasing the autophagic cell population to 87.6 × 103 cells compared to 32.8 × 103 in the control.
体内研究
(In Vivo)

Pim-1 kinase inhibitor 8 (5 mg/kg，腹腔注射，每日给药，持续 24 天) 在实体艾氏腹水癌 (SEC) 荷瘤小鼠中表现出肿瘤抑制活性[1]。

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

Animal Model: Adult female Swiss albino mice (18-23 g) subcutaneously injected with SEC cells[1]
Dosage: 5 mg/kg
Administration: i.p., daily for 24 days
Result: Decreased tumor weight from 198.5 mg in control to 72.8 mg.
Reduced tumor volume from 274.8 mm3 in the untreated control to 159.2 mm3.
Greatly decreased tumor proliferation by 42.1 %.
分子量

275.30

Formula

C14H17N3O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (454.05 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6324 mL 18.1620 mL 36.3240 mL
5 mM 0.7265 mL 3.6324 mL 7.2648 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Pim-1 kinase inhibitor 8 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6324 mL 18.1620 mL 36.3240 mL 90.8100 mL
5 mM 0.7265 mL 3.6324 mL 7.2648 mL 18.1620 mL
10 mM 0.3632 mL 1.8162 mL 3.6324 mL 9.0810 mL
15 mM 0.2422 mL 1.2108 mL 2.4216 mL 6.0540 mL
20 mM 0.1816 mL 0.9081 mL 1.8162 mL 4.5405 mL
25 mM 0.1453 mL 0.7265 mL 1.4530 mL 3.6324 mL
30 mM 0.1211 mL 0.6054 mL 1.2108 mL 3.0270 mL
40 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2703 mL
50 mM 0.0726 mL 0.3632 mL 0.7265 mL 1.8162 mL
60 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5135 mL
80 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1351 mL
100 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9081 mL
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:

Pim-1 kinase inhibitor 8916038-47-6PimApoptosisAutophagyPim kinasesPim-1 kinaseantiproliferationmigrationapoptosissolid tumorbreast cancerMCF-7HepG2liver cancerInhibitorinhibitorinhibit

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