P6624

PS-1145 dihydrochloride

≥98% (HPLC), solid

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

Properties

• 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

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[1]
• 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[2]
• to examine the involvement of NF-κB signaling in the cytotoxic effect of niclosamide on colorectal cancer (CRC) cells[3]

Biochem/physiol Actions

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

PS-1145, a β-carboline derivative,[4] 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.[4]

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.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H302
• pcodes: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: dust mask type N95 (US), Eyeshields, Gloves