2. NF-κB
  3. NF-κB
  4. IT-901

IT-901 是一种具有口服活性且有效的 NF-κB 亚基 c-Rel 抑制剂，对 NF-κB 和 c-Rel 与 DNA 结合的 IC50 分别为 0.1 µM，3 μM。IT-901 是一种具有生物活性的萘硫代巴比妥酸酯衍生物，具有用于人类淋巴瘤和改善移植物抗宿主病 (GVHD) 的潜力。

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IT-901 Chemical Structure

IT-901 Chemical Structure

CAS No. : 1584121-99-2

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规格 价格 是否有货 数量
1 mg ￥1590
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5 mg ￥3500
In-stock
10 mg ￥5600
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100 mg   询价  

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Customer Review

IT-901 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD)[1][2].

IC50 & Target[1]

c-Rel

3 μM (IC50)

NF-κB

0.1 μM (IC50)

体外研究
(In Vitro)

IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells[1].
IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1[1].
IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines[2].
The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM[1].
The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells[1].
IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC50 values between 3μM to 4μM[1].

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

IT-901 相关抗体:

Cell Proliferation Assay[1]

Cell Line: TMD8 and SU-DHL8 cells
Concentration: 1, 3, 5 μM
Incubation Time: For 24 hours
Result: Resulted in decreased proliferation of viable ABC and GCB DLBCL cells.

Cell Viability Assay[1]

Cell Line: SU-DHL8 and TMD8 cells
Concentration: 3 μM
Incubation Time: For 24 hours
Result: Decreased cell viability in a dose-dependent fashion.

Western Blot Analysis[2]

Cell Line: Primary chronic lymphocytic leukemia (CLL) cells and cell lines
Concentration: 1, 5, 10 μM
Incubation Time: For 6 hours
Result: Documented Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreased the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms.
体内研究
(In Vivo)

IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity[1].
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax[1].

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

Animal Model: BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old[1]
Dosage: 24 mg/kg
Administration: IP; every other day for 2 weeks
Result: Had an effective treatment of acute GVHD without impairing anti-tumor activity.
分子量

342.37

Formula

C17H14N2O4S
CAS 号
性状

固体

颜色

Orange to red

运输条件

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

DMSO 中的溶解度 : 12.5 mg/mL (36.51 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 2.9208 mL 14.6041 mL 29.2082 mL
5 mM 0.5842 mL 2.9208 mL 5.8416 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

纯度: ≥99.0%

COA (265 KB)

产品使用指南 (1538 KB)
参考文献

IT-901 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 2.9208 mL 14.6041 mL 29.2082 mL 73.0204 mL
5 mM 0.5842 mL 2.9208 mL 5.8416 mL 14.6041 mL
10 mM 0.2921 mL 1.4604 mL 2.9208 mL 7.3020 mL
15 mM 0.1947 mL 0.9736 mL 1.9472 mL 4.8680 mL
20 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6510 mL
25 mM 0.1168 mL 0.5842 mL 1.1683 mL 2.9208 mL
30 mM 0.0974 mL 0.4868 mL 0.9736 mL 2.4340 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:

IT-9011584121-99-2IT901IT 901NF-κBNuclear factor-κBNuclear factor-kappaBorallyDNAbindingnaphthalenethiobarbituratederivativehumanlymphoidtumorsameliorategraft-versus-hostdiseaseGVHDInhibitorinhibitorinhibit

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目录号：
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