P6624
PS-1145 dihydrochloride
≥98% (HPLC), solid
Synonyme(s) :
N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
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A propos de cet article
Formule empirique (notation de Hill) :
C17H11ClN4O · 2HCl
Numéro CAS:
Poids moléculaire :
395.67
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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Laissez-nous vous aiderInChI 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
Catégories apparentées
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
Classe de stockage
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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A Yemelyanov et al.
Oncogene, 25(3), 387-398 (2005-09-20)
A key antiapoptotic transcription factor, nuclear factor kappa-B (NF-kappaB), is known to be critically important for tumor cell growth, angiogenesis and development of metastatic lesions. We and others showed previously that NF-kappaB transcription factor was constitutively activated in androgen-independent prostate
Lloyd T Lam et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(1), 28-40 (2005-01-27)
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
Takuya Osada et al.
Cancer research, 71(12), 4172-4182 (2011-05-03)
Wnt/β-catenin pathway activation caused by adenomatous polyposis coli (APC) mutations occurs in approximately 80% of sporadic colorectal cancers (CRC). The antihelminth compound niclosamide downregulates components of the Wnt pathway, specifically Dishevelled-2 (Dvl2) expression, resulting in diminished downstream β-catenin signaling. In
Martina Kunkl et al.
Frontiers in immunology, 11, 590964-590964 (2020-11-13)
IL-22 is a member of the IL-10 cytokine family involved in host protection against extracellular pathogens, by promoting epithelial cell regeneration and barrier functions. Dysregulation of IL-22 production has also frequently been observed in acute respiratory distress syndrome (ARDS) and
Jianghua Wang et al.
Cancer research, 71(4), 1325-1333 (2010-12-21)
The TMPRSS2/ERG (T/E) fusion gene is present and thought to be an oncogenic driver of approximately half of all prostate cancers. Fusion of the androgen-regulated TMPRSS2 promoter to the ERG oncogene results in constitutive high level expression of ERG which
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