P6624

PS-1145 dihydrochloride

≥98% (HPLC), solid

• Synonym(e): N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
• Empirische Formel (Hill-System): C₁₇H₁₁ClN₄O · 2HCl
• CAS-Nummer: 431898-65-6
• Molekulargewicht: 395.67
• NACRES: NA.77
• PubChem Substance ID: 24724584
• UNSPSC Code: 12352200
• MDL number: MFCD08705411
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: desiccated

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• storage condition: desiccated
• color: yellow
• solubility: 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.)
• storage temp.: 2-8°C
• SMILES string: 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

Beschreibung

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

Biochem/physiol Actions

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.

Features and Benefits

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

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H302
• Sicherheitshinweise: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• PSA (Persönliche Schutzausrüstung): dust mask type N95 (US), Eyeshields, Gloves