|PS 1145 2HCl|CsnPharm

CAS No.: 1049743-58-9

PS-1145 2HCl Catalog No. CSN23053

PS 1145 2HCl is a selective IκB kinase (IKK) inhibitor with IC50 of 100 nM.

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技术信息

生物活性

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 2HCl is the dihydrochlorde form of PS 1145. 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^[1] (i.v.) Rat: 50 mg/kg^[2] (i.v.)

给药途径
i.v.

动物研究
剂量	Mice: 3 mg/kg^[1] (i.v.) Rat: 50 mg/kg^[2] (i.v.)
给药途径	i.v.

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
- 2.5274 mL
- 12.6368 mL
- 25.2736 mL
- 5 mM
- 0.5055 mL
- 2.5274 mL
- 5.0547 mL
- 10 mM
- 0.2527 mL
- 1.2637 mL
- 2.5274 mL

技术信息

CAS号	1049743-58-9	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C17H13Cl3N4O	运输	蓝冰
分子量	395.67	别名

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PS-1145 2HCl Catalog No. CSN23053

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