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P6624

Sigma-Aldrich

PS-1145 dihydrochloride

≥98% (HPLC), solid

Szinonimák:

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

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About This Item

Tapasztalati képlet (Hill-képlet):
C17H11ClN4O · 2HCl
CAS-szám:
431898-65-6
Molekulatömeg:
395.67
MDL-szám:
MFCD08705411
UNSPSC kód:
12352200
PubChem Substance ID:
24724584
NACRES:
NA.77

Minőségi szint

100

Teszt

≥98% (HPLC)

Forma

solid

tárolási körülmény

desiccated

szín

yellow

oldhatóság

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.)

tárolási hőmérséklet

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

Nemzetközi kémiai azonosító kulcs

QTDCBADLGJZBHP-UHFFFAOYSA-N

Alkalmazás

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

Biokémiai/fiziológiai hatások

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.

Tulajdonságok és előnyök

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

Piktogramok

Exclamation mark
GHS07

Figyelmeztetés

Warning

Figyelmeztető mondatok

H302

Óvintézkedésre vonatkozó mondatok

P264 - P270 - P301 + P312 - P501

Veszélyességi osztályok

Acute Tox. 4 Oral

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

Egyéni védőeszköz

dust mask type N95 (US), Eyeshields, Gloves

Válasszon a legfrissebb verziók közül:

Analitikai tanúsítványok (COA)

Lot/Batch Number
0000167415
0000141781
083M4617V
050M4603
099K4614

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Dokumentumtár megtekintése

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
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
View All Related Papers

Cikkek

MAPKKKs

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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