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PS-1145 dihydrochloride

SIGMA/P6624 - ≥98% (HPLC), solid

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

CAS Number: 431898-65-6 (free base)
Empirical Formula (Hill Notation): C17H11ClN4O · 2HCl
Molecular Weight: 395.67
MDL Number: MFCD08705411
Linear Formula: C17H11ClN4O · 2HCl
Product Type: Chemical

Catalog Number PKG Qty. Price Quantity
45-P6624-5MG 5 mg
$200.00
1/EA
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45-P6624-25MG 25 mg
$577.00
1/EA
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assay ≥98% (HPLC)
color yellow
form solid
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
Quality Level 100 
SMILES string Cl[H].Cl[H].Clc1cc(NC(=O)c2cccnc2)c3[nH]c4cnccc4c3c1
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 condition desiccated
storage temp. 2-8°C
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 is an IKB kinase (IKK) inhibitor.
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.
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 .
Packaging: 5, 25 mg in glass bottle
Symbol GHS07  GHS07
Signal word Warning
Hazard statements H302
Hazard Codes Xn
Risk Statements 22
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352200

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