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Merck
모든 사진(1)

주요 문서

P6624

Sigma-Aldrich

PS-1145 dihydrochloride

≥98% (HPLC), solid

동의어(들):

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

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About This Item

실험식(Hill 표기법):
C17H11ClN4O · 2HCl
CAS Number:
Molecular Weight:
395.67
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

solid

저장 조건

desiccated

색상

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.)

저장 온도

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

애플리케이션

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

생화학적/생리학적 작용

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.

특징 및 장점

This compound is featured on the MAPKKKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

예방조치 성명서

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

dust mask type N95 (US), Eyeshields, Gloves


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문서 라이브러리 방문

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
Sameek Roychowdhury et al.
Journal of the National Cancer Institute, 96(19), 1447-1457 (2004-10-07)
Immune-compromised individuals are at increased risk for developing aggressive Epstein-Barr virus (EBV)-associated lymphoproliferative disorders after primary EBV infection or for reactivation of a preexisting latent EBV infection. We evaluated the effect of depsipeptide, a histone deacetylase inhibitor, on EBV-positive lymphoblastoid
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
Ian C Henrich et al.
Cancer research, 81(8), 2171-2183 (2021-02-10)
Ewing sarcoma is the second most common pediatric bone cancer, with a 5-year survival rate for metastatic disease of only 20%. Recent work indicates that survival is strongly correlated with high levels of tumor-infiltrating lymphocytes (TIL), whose abundance is associated
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

문서

The extracellular signal regulated kinase (ERK1 and ERK2) pathways are activated by mitogens and play an important role in controlling cell growth and differentiation.

The extracellular signal regulated kinase (ERK1 and ERK2) pathways are activated by mitogens and play an important role in controlling cell growth and differentiation.

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