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CAS No.: 431898-65-6

PS-1145 Catalog No. CSN18270

Synonyms: IKK Inhibitor X

PS-1145 is an IkappaB kinase (IKK) inhibitor with IC50 of 88 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 IKK

IC50:88nM
描述The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. The activation of the upstream molecule, IKKα or β (IkB kinase), is required for NF-kB pathway and regulates NF-kB pathway via phosphorylation by specific IKK kinases and by autophosphorylation. PS-1145 is an IKK inhibitor with IC50 value of 88nM (measured by kinase activity). Through inhibition of IKK, pre-treatment with 10μM PS-1145 for 90 min strongly inhibited TNFα-induced phosphorylation and degradation of IκBα, as well as the subsequent NF-κB-DNA binding in MM.1S cells at 10 or 20 minutes after TNFα treatment. 20–50% proliferative inhibition can be observed in MM.1S, U266, and RPMI8226 cell lines cultures for 48 hours in the presence of PS-1145 at concentration ranging in 1.5–50μM. Meanwhile, the enhanced apoptosis could be observed in MM.1S cells treated with 1ng/ml TNFα in the presence of 10μM PS-1145 due to its effect on inhibition of the NF-κB pathway and TNFα-induced up-regulation of ICAM-1 expression. Both constitutive secretion of IL-6 in BMSCs and increased IL-6 secretion triggered by adhesion of MM.1S cells to BMSCs can be blocked by PS-1145 at concentration ranging in 0.4-10μM in a dose-dependent fashion. PS-1145 (8 μM) was able to suppress T-cell alloreactivity in vitro and induce apoptosis though it was less potent than bortezomib (0.32μM). However, compared with bortezomib, PS-1145 (50 mg/kg, i.p.) showed no early toxicity in prolonged treatment in a bone marrow transplantation study and showed more complete protection against lethal graft-versus-host disease (GVHD).
动物研究
剂量
Mice: 3 mg/kg^[3] (i.v.); 0.5 mg/kg - 500 mg/kg^[4] (p.o.) Rat: 50 mg/kg^[5] (i.v.)

给药途径
i.v., p.o.
参考文献

动物研究
剂量	Mice: 3 mg/kg^[3] (i.v.); 0.5 mg/kg - 500 mg/kg^[4] (p.o.) Rat: 50 mg/kg^[5] (i.v.)
给药途径	i.v., p.o.

[1] Lupino E, Ramondetti C, Piccinini M. IκB kinase β is required for activation of NF-κB and AP-1 in CD3/CD28-stimulated primary CD4(+) T cells. J Immunol. 2012 Mar 15;188(6):2545-55.
[2] Hideshima T, Chauhan D, et al. NF-kappa B as a therapeutic target in multiple myeloma. J Biol Chem. 2002 May 10;277(19):16639-47.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0984 mL
- 15.4919 mL
- 30.9839 mL
- 5 mM
- 0.6197 mL
- 3.0984 mL
- 6.1968 mL
- 10 mM
- 0.3098 mL
- 1.5492 mL
- 3.0984 mL

技术信息

CAS号

431898-65-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H11ClN4O

运输

蓝冰

分子量

322.75

别名

IKK Inhibitor X

溶解度

DMSO	64.0 mg/mL (198.3 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (6.2 mM) warming

动物实验配方

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PS-1145 Catalog No. CSN18270

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