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PS-1145

目录号: PC11576 纯度: ≥98%

IKK抑制剂，PS-1145 是一种 IκB 激酶 (IKK) 抑制剂，IC50 为 88 nM。

CAS No. :431898-65-6

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中文名称

PS-1145

中文别名

N-(6-氯-9H-吡啶并[3,4-b]吲哚-8-基)-3-吡啶甲酰胺

英文名称

PS-1145

英文别名

PS 1145;PS-1145;N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide;N-(6-CHLORO-9H-PYRIDO[3,4-B]INDOL-8-YL)-3-PYRIDINECARBOXAMIDE DIHYDROCHLORIDE;N-(6-Chloro-9H-beta-carbolin-8-yl)-nicotinamide;N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)nicotinamide;3-Pyridinecarboxamide, N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)-;N-{6-chloro-9H-pyrido[3,4-b]indol-8-yl}pyridine-3-carboxamide;IKK Inhibitor X;MLS006010310;JZRMBDHPALEPDM-UHFFFAOYSA-N;HMS3748G21;HMS3229F21;BCP24095;MFC;N-(6-Chloro-9h-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide;BC

Cas No.

431898-65-6

分子式

C₁₇H₁₁ClN₄O

分子量

322.75

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

IKK抑制剂，PS-1145 是一种 IκB 激酶 (IKK) 抑制剂，IC50 为 88 nM。

生物活性

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

性状

Solid

IC50 & Target[1][2]

IKK

88 nM (IC₅₀)

体外研究(In Vitro)

PS-1145 blocks TNFα-induced NF-κB activation in a dose- and time-dependent fashion in MM cells through inhibition of IκBα phosphorylation. Dexamethasone (Dex), which up-regulates IκBα protein, enhances blockade of NF-κB activation by PS-1145. PS-1145 blocks the protective effect of IL-6 against Dex-induced apotosis. TNFα-induced intracellular adhesion molecule (ICAM)-1 expression on both RPMI8226 and MM.1S cells is also inhibited by PS-1145. Moreover, PS-1145 inhibits both IL-6 secretion from bone marrow stromal cells (BMSCs) triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs.

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

体内研究(In Vivo)

Administration of either Bortezomib or PS-1145 (50 mg/kg) results in a significant decrease in serum levels of all 3 cytokines that is nonsignificantly different from those in mice that underwent transplantation with TCD BM alone. PS1145 is injected intracerebroventricular (icv) as a pretreatment to block hypothalamic inflammation induced by IL-4 in adult male Wistar rats consuming a high-fat diet (HFD) over an 11-day period. The four groups of rats according to icv pretreatment/treatment condition are Veh/Veh, Veh/IL-4, PS1145/Veh, and PS1145/IL-4. Rats in the Veh/IL-4 group display increased weight gain on the HFD compared with the Veh/Veh group (P<0.05 on days 6-9). Importantly, the effect of icv IL-4 administration to increase body fat mass during high-fat (HF) feeding is completely blocked by icv PS1145 pretreatment at a dose that has no independent effect on body composition (on day 8: P<0.001, PS1145/Veh vs. PS1145/IL-4; P=not significant, PS1145/Veh vs. Veh/Veh). In PS1145/IL-4 injected rats, IL-1β mRNA content is decreased by ~75% compared with that of Veh/IL-4-injected rats.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Hideshima T, et al. NF-kappa B as a therapeutic target in multiple myeloma. J Biol Chem. 2002 May 10;277(19):16639-47. [Information]

[2]. Vodanovic-Jankovic S, et al. NF-kappaB as a target for the prevention of graft-versus-host disease: comparative efficacy of bortezomib and PS-1145. Blood. 2006 Jan 15;107(2):827-34. [Information]

[3]. Oh-I S, et al. Central administration of interleukin-4 exacerbates hypothalamic inflammation and weight gain during high-fat feeding. Am J Physiol Endocrinol Metab. 2010 Jul;299(1):E47-53. [Information]

溶解度数据

体外研究:

DMSO : 20.83 mg/mL (64.54 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0984 mL	15.4919 mL	30.9837 mL
5 mM	0.6197 mL	3.0984 mL	6.1967 mL
10 mM	0.3098 mL	1.5492 mL	3.0984 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (6.44 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.44 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.44 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.44 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Hideshima T, et al. NF-kappa B as a therapeutic target in multiple myeloma. J Biol Chem. 2002 May 10;277(19):16639-47. [Information]

[2]. Vodanovic-Jankovic S, et al. NF-kappaB as a target for the prevention of graft-versus-host disease: comparative efficacy of bortezomib and PS-1145. Blood. 2006 Jan 15;107(2):827-34. [Information]

[3]. Oh-I S, et al. Central administration of interleukin-4 exacerbates hypothalamic inflammation and weight gain during high-fat feeding. Am J Physiol Endocrinol Metab. 2010 Jul;299(1):E47-53. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

PS-1145

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