1. Immunology/Inflammation Apoptosis
  2. AP-1 Apoptosis
  3. INI-43

INI-43 是 Kpnβ1 的抑制剂,干扰 Kpnβ1 和已知的 Kpnβ1 cargo 蛋白、NFAT、NFκB、AP-1和 NFY 的核定位。INI-43 能抑制癌细胞的增殖,在癌细胞中引起 G2-M 细胞周期阻滞,并诱导细胞内在凋亡 (apoptosis) 途径。

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INI-43 Chemical Structure

INI-43 Chemical Structure

CAS No. : 881046-01-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1650
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1 mg ¥600
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5 mg ¥1500
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10 mg ¥2500
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25 mg ¥5500
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50 mg ¥9500
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200 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G2-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway[1][2][3].

体外研究
(In Vitro)

INI-43 (5 μM, 2h) 在宫颈癌 HeLa 和 SiHa 细胞株中预处理能够有效减少 NFκB 的核积累并降低其活性,导致 cyclin D1、c-Myc 和 XIAP 的表达下降,DNA 修复能力受损,使细胞对 Cisplatin (HY-17394) 更敏感[2]
INI-43 (10, 15 μmol/L, 1.5, 3h) 在 HeLa 细胞中具有干扰 Kpnβ1, NFAT, p65 和 NFY 进入核内,以及诱导细胞凋亡 (apoptosis) 的作用。INI-43 对 HeLa 细胞的 IC50 值为 9.3 μmol/L[3]
INI-43 (5, 10 μmol/L, 5天) 对癌细胞系 (宫颈癌和食管癌) 和非癌细胞系 (DMB 和 FG0) 的敏感性不同,INI-43 能杀伤癌细胞,对非癌细胞无影响[3]

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

Cell Proliferation Assay[3]

Cell Line: CaSki, HeLa, Kyse30, WHCO6, DMB and FG0 cells
Concentration: 5, 10 μmol/L
Incubation Time: 5 days
Result: At a concentration of 10 μmol/L, in less than 24 hours, the activity of cancer cells was significantly reduced, and within 48 to 72 hours, the cells were completely dead.

Western Blot Analysis[3]

Cell Line: HeLa cells
Concentration: 10, 15 μmol/L
Incubation Time: 1.5, 3h
Result: Prevented NFY from entering the nucleus.
Cytochrome C levels in mitochondria decreased, activating endogenous apoptotic pathways, and caspase-3/7 activity significantly increased.

Western Blot Analysis[2]

Cell Line: HeLa and SiHa cells
Concentration: 5 μM
Incubation Time: 2h
Result: Has a synergistic effect with Cisplatin, can inhibit Kpnβ1, increase the stability of p53, reduce the nuclear localization of NFκB and its target expression in SiHa cells after Cisplatin treatment, and enhance the DNA damage after Cisplatin treatment.

Immunofluorescence[3]

Cell Line: HeLa cells
Concentration: 10 μmol/L
Incubation Time: 1.5, 3h
Result: Prevented p65 from entering the nucleus.
体内研究
(In Vivo)

INI-43 在小鼠肿瘤异种移植模型中具有良好的代谢稳定性,降解半衰期超过 100 分钟, 最大耐受剂量 (MTD) 为 50 mg/kg[3]
INI-43 (50 mg/kg,腹腔注射, 2-3 天一次,持续 3-4 周) 在食管癌细胞 (WHCO6) 和宫颈癌细胞 (CaSki) 异种移植瘤小鼠模型中具有抑制肿瘤生长的作用[3]

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

Animal Model: WHCO6 esophageal cancer or CaSki cervical cancer cells mouse xenografts models[3]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Significantly inhibited the growth of esophageal and neck tumors.
分子量

385.46

Formula

C22H23N7

CAS 号
性状

固体

颜色

Light yellow to yellow

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
In Vitro: 

DMSO 中的溶解度 : 10 mg/mL (25.94 mM; 超声助溶 (<60°C); 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 2.5943 mL 12.9715 mL 25.9430 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 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

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

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 2.5943 mL 12.9715 mL 25.9430 mL 64.8576 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 mL 12.9715 mL
10 mM 0.2594 mL 1.2972 mL 2.5943 mL 6.4858 mL
15 mM 0.1730 mL 0.8648 mL 1.7295 mL 4.3238 mL
20 mM 0.1297 mL 0.6486 mL 1.2972 mL 3.2429 mL
25 mM 0.1038 mL 0.5189 mL 1.0377 mL 2.5943 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.

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产品名称:
INI-43
目录号:
HY-121607
需求量: