P6624
PS-1145 dihydrochloride
≥98% (HPLC), solid
Sinónimos:
N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
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Acerca de este artículo
Fórmula empírica (notación de Hill):
C17H11ClN4O · 2HCl
Número CAS:
Peso molecular:
395.67
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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Permítanos ayudarleNombre del producto
PS-1145 dihydrochloride, ≥98% (HPLC), solid
InChI key
QTDCBADLGJZBHP-UHFFFAOYSA-N
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
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
Quality Level
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.
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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Journal of the National Cancer Institute, 96(19), 1447-1457 (2004-10-07)
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Constitutive activation of the NF-kappaB pathway is required for survival of the activated B cell-like (ABC) subgroup of diffuse large B-cell lymphoma (DLBCL). Here we show that a small molecule IkappaB kinase (IKK) inhibitor, PS-1145, and related compounds are toxic
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