PS-1145 二盐酸盐

Name: PS-1145 二盐酸盐
Brand: SIGMA

≥98% (HPLC), solid

别名:

N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride

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所有图片(1)

About This Item

经验公式（希尔记法）:

C₁₇H₁₁ClN₄O · 2HCl

CAS Number:

431898-65-6

分子量:

395.67

MDL编号:

MFCD08705411

UNSPSC代码:

12352200

PubChem化学物质编号:

24724584

NACRES:

NA.77

质量水平

100

方案

≥98% (HPLC)

表单

solid

储存条件

desiccated

颜色

yellow

溶解性

DMSO: >3 mg/mL at ~60 °C, clear (with warming for 2 minutes)
methanol: water (1:1): ≥5 mg/mL at 60 °C (With warming for 5 minutes.)

储存温度

2-8°C

SMILES字符串

Cl[H].Cl[H].Clc1cc(NC(=O)c2cccnc2)c3[nH]c4cnccc4c3c1

InChI

1S/C17H11ClN4O.2ClH/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10;;/h1-9,21H,(H,22,23);2*1H

InChI key

QTDCBADLGJZBHP-UHFFFAOYSA-N

应用

PS-1145 dihydrochloride has been used as an IκB kinase (IKK) inhibitor:

in the culture medium to treat human epidermal keratinocytes (HEKs) and squamous carcinoma cells (SCCs) to study the role of IKK in Corynebacterium tuberculostearicum (C. t.)-elicited transcription of inflammatory mediators
to investigate the involvement of transcription factor p65 (RelA)/nuclear factor kappa-B (NF-κB) in the cluster of differentiation 28 (CD28)-mediated interleukin-17A (IL-17A) gene expression
to examine the involvement of NF-κB signaling in the cytotoxic effect of niclosamide on colorectal cancer (CRC) cells

生化/生理作用

PS-1145 is an IKB kinase (IKK) inhibitor.

PS-1145, a β-carboline derivative, blocks the phosphorylation and degradation of the inhibitor of nuclear factor kappa-β (NF-κB;). It also inhibits the subsequent activation of nuclear factor kappa-β (NF-κB) and thereby prevents the release of tumor necrosis factor-α (TNF-α) in lipopolysaccharide treated mice. PS-1145 hinders pro-inflammatory cytokine production and cell proliferation. It plays a potential therapeutic role in carcinogenesis in multiple myeloma. PS-1145 exhibits anti-tumor activity on nasopharyngeal carcinoma (NPC) cell lines.

特点和优势

This compound is featured on the MAPKKKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.