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Merck
모든 사진(1)

주요 문서

SML0766

Sigma-Aldrich

GSK343

≥98% (HPLC)

동의어(들):

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide, N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-(propan-2-yl)-1H-indazole-4-carboxamide

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About This Item

실험식(Hill 표기법):
C31H39N7O2
CAS Number:
Molecular Weight:
541.69
MDL number:
UNSPSC 코드:
41106514
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

, white to beige to brown

solubility

DMSO: 15 mg/mL, clear

저장 온도

2-8°C

SMILES string

CN(CC1)CCN1C2=NC=CC(C3=CC4=C(C=NN4C(C)C)C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)=C2

InChI

1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)

InChI key

ULNXAWLQFZMIHX-UHFFFAOYSA-N

애플리케이션

GSK343 has been used:
  • as an inhibitor of enhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation on cell migration
  • as histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCR reporter gene expression, facilitated by TC14-3
  • as a supplement in the growth medium to inhibit the generation of H3K27me3 or to inhibit RNA polymerase II
  • as EZH2 inhibitor to treat castration-resistant neuroendocrine prostate cancer (CRPC-NE)

생화학적/생리학적 작용

GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC50 for inhibition of H3K27 methylation is < 200 nM in HCC1806 cells. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

특징 및 장점

GSK343 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

기타 정보

GSK343 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK343 probe summary on the Chemical Probes Portal website.

관련 제품

제품 번호
설명
가격

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


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문서

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

관련 콘텐츠

당사는 유전자 조절 연구 분야에서 표적 식별 및 검증을 위해 전사 인자 조절인자, 염색질 변형 효소 억제제, 작용제/길항제와 같은 여러 저분자 연구 툴을 제공합니다. 이러한 연구 툴 제품군은 아래에 나와 있습니다.

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