P6624

PS-1145 dihydrochloride

≥98% (HPLC), solid

• Synonyme(s) : N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
• Formule empirique (notation de Hill): C₁₇H₁₁ClN₄O · 2HCl
• Numéro CAS: 431898-65-6
• Poids moléculaire : 395.67
• Numéro MDL: MFCD08705411
• Code UNSPSC : 12352200
• ID de substance PubChem : 24724584
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Conditions de stockage: desiccated
• Couleur: yellow
• Solubilité: 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.)
• Température de stockage: 2-8°C
• Chaîne SMILES: 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
• Clé InChI: QTDCBADLGJZBHP-UHFFFAOYSA-N

Description

Application

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

Actions biochimiques/physiologiques

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.

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

Caractéristiques et avantages

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

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: dust mask type N95 (US), Eyeshields, Gloves