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P6624

PS-1145 dihydrochloride

Name: PS-1145 dihydrochloride
Brand: SIGMA

≥98% (HPLC), solid

Sinónimos:

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

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Fórmula empírica (notación de Hill):

C₁₇H₁₁ClN₄O · 2HCl

Número CAS:

431898-65-6

Peso molecular:

395.67

NACRES:

NA.77

PubChem Substance ID:

24724584

UNSPSC Code:

12352200

MDL number:

MFCD08705411

Assay:

≥98% (HPLC)

Form:

solid

Storage condition:

desiccated

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Propiedades

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

Descripción

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.

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Este artículo	D0444	O9890	C6617
Sigma-Aldrich P6624 PS-1145 dihydrochloride	Sigma-Aldrich D0444 DT-2 trifluoroacetate salt	Sigma-Aldrich O9890 5Z-7-Oxozeaenol	Sigma-Aldrich C6617 CBIQ
description ≥98% (HPLC), solid	description ≥95% (HPLC), film	description ≥98% (HPLC)	description ≥98% (HPLC), solid
assay ≥98% (HPLC)	assay ≥95% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form solid	form film	form powder	form solid
Quality Level 100	Quality Level 200	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. −20°C	storage temp. 2-8°C	storage temp. -
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.)	solubility H₂O: 0.5 mg/mL, clear	solubility DMSO: >10 mg/mL	solubility DMSO: 15 mg/mL
storage condition desiccated	storage condition -	storage condition -	storage condition -