P6624

PS-1145 二塩酸塩

≥98% (HPLC), solid

• 別名: N-(6-クロロ-9H-ピリド[3,4-b]インドール-8-イル)-3-ピリジンカルボキサミド 二塩酸塩
• 実験式（ヒル表記法）: C₁₇H₁₁ClN₄O · 2HCl
• CAS番号: 431898-65-6
• 分子量: 395.67
• MDL番号: MFCD08705411
• UNSPSCコード: 12352200
• PubChem Substance ID: 24724584
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: solid
• 保管条件: desiccated
• 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.)
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

アプリケーション

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

生物化学的／生理学的作用

IKBキナ-ゼ (IKK) インヒビタ-。

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.

特徴および利点

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

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H302
• 注意書き: P264 - P270 - P301 + P312 - P501
• 危険有害性の分類: Acute Tox. 4 Oral
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable
• 個人用保護具 (PPE): dust mask type N95 (US), Eyeshields, Gloves