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Merck
모든 사진(1)

주요 문서

SML1684

Sigma-Aldrich

GSK2850163

≥98% (HPLC)

동의어(들):

(R)-2-(3,4-Dichlorobenzyl)-N-(4-methylbenzyl)-2,7-diazaspiro[4.5]decane-7-carboxamide

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크기 선택

5 MG
120,00 €
25 MG
483,00 €

120,00 €


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5 MG
120,00 €
25 MG
483,00 €

About This Item

실험식(Hill 표기법):
C24H29Cl2N3O
CAS Number:
Molecular Weight:
446.41
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

120,00 €


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Quality Level

분석

≥98% (HPLC)

양식

oil

색상

colorless to light yellow

저장 온도

2-8°C

SMILES string

ClC1=CC(CN(C2)CC[C@]32CN(C(NCC4=CC=C(C)C=C4)=O)CCC3)=CC=C1Cl

InChI

1S/C24H29Cl2N3O/c1-18-3-5-19(6-4-18)14-27-23(30)29-11-2-9-24(17-29)10-12-28(16-24)15-20-7-8-21(25)22(26)13-20/h3-8,13H,2,9-12,14-17H2,1H3,(H,27,30)/t24-/m1/s1

InChI key

YFDASBFQKMHSSJ-XMMPIXPASA-N

유사한 품목 비교

전체 비교 보기

차이점 표시

1 of 4

이 품목
SML1297SML1998SML1506
GSK2850163 ≥98% (HPLC)

SML1684

GSK2850163

SB269652 ≥98% (HPLC)

SML1297

SB269652

KLH45 ≥98% (HPLC)

SML1998

KLH45

KY-05009 ≥98% (HPLC)

SML1506

KY-05009

form

oil

form

powder

form

oil

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

color

colorless to light yellow

color

white to beige

color

colorless to light yellow

color

light yellow to dark yellow

생화학적/생리학적 작용

GSK2850163 is a highly selective inhibitor of inositol requiring enzyme-1 alpha (IRE1α) with dual activity: it inhibits IRE1α kinase activity with an IC50 value of 20 nM and RNase activity with an IC50 value of 200 nM. IRE1α is a dual serine/threonine-protein kinase/endoribonuclease with two enzymatic domains: a trans-autophosphorylation domain and and endoribonuclease (RNase) domain. When activated, usually in response to endoplasmic reticulum (ER) stress such as the unfolded protein response (UPR), IRE1α oligomerizes and activates mRNA splicing of adaptive XBP1 transcription factor, which upregulates ER chaperones and ER associated degradation (ERAD) genes that promote degradation of ER unfolded proteins and facilitate recovery from ER stress. However, if ER stress is too high or chronic, IRE1α is hyperactivated, increasing many ER mRNAs, resulting in apoptosis. GSK2850163 interacts with IRE1α catalytic residues Lys599 and Glu612, displacing the kinase activation loop to the inactive DFG-out conformation. The rearrangement of the kinase domain-dimer interface also results in the RNAse domains rotating away from each other, inhibiting the RNase activity.
IRE1α-selective inhibitor of XBP1 splicing
IRE1α-selective inhibitor of XBP1 splicing.
Homoharringtonine is a cephalotaxine ester that is also known as (HHT; 4-methyl (2R)-2-hydroxy-2-(4-hydroxy-4-methylpentyl)butanedioate). In gefitinib-resistant lung cancer cells, homoharringtonine promotes apoptosis and prevents signal transducer and activator of transcription (STAT3) through IL-6 (interleukin-6) /JAK1 (janus kinase 1)/STAT3 signal pathway.[1] It plays an important role in the treatment of malaria.[2]

유해 및 위험 성명서

예방조치 성명서

Hazard Classifications

Aquatic Chronic 4

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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    이미 열람한 고객

    Chemistry and Biology, 439-439 (1998)
    Wei Cao et al.
    Scientific reports, 5, 8477-8477 (2015-07-15)
    Tyrosine kinase inhibitors (TKIs) are mostly used in non-small cell lung cancer (NSCLC) treatment. Unfortunately, treatment with Gefitinib for a period of time will result in drug resistance and cause treatment failure in clinic. Therefore, exploring novel compounds to overcome

    자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

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