PFI-2 (hydrochloride)

PFI-2 (hydrochloride) 구조식 이미지
카스 번호:
1627607-87-7
상품명:
PFI-2 (hydrochloride)
동의어(영문):
(R)-PFI-2;PFI-2 HCl salt;PFI-2 (hydrochloride);(R)-PFI-2 (hydrochloride);PFI-2; PFI2;PFI 2;R PFI-2;R-PFI2;(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride;(R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride;macrophage,chronic kidney disease,inhibit,Histone Methyltransferase,PFI-2,Inhibitor,SET domain containing lysine methyltransferase 7 (SETD7),PFI2 hydrochloride,renal fibrosis,inflammation,PFI 2,PFI2,PFI 2 hydrochloride
CBNumber:
CB83041444
분자식:
C23H26ClF4N3O3S
포뮬러 무게:
535.98
MOL 파일:
1627607-87-7.mol
MSDS 파일:
SDS

PFI-2 (hydrochloride) 속성

녹는점
>209°C (dec.)
저장 조건
2-8°C
용해도
DMSO에 용해됨(최대 25mg/ml)
물리적 상태
가루
색상
흰색에서 베이지색
안정성
제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 2개월 동안 보관할 수 있습니다.
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
예방조치문구:

PFI-2 (hydrochloride) C화학적 특성, 용도, 생산

개요

SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage as well as the transcription factor TAF10. (R)-PFI-2 is a potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases. Its enantiomer, (S)-PFI-2 , is 500-fold less active (IC50 = 1 μM). See the Structural Genomics Consortium (SGC) website for more information.

용도

(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide Hydrochloride known as (-)-PFI-2 HCl is a cell permeable inhibitor of SET Domain-Containing protein 7/9 (SET 7/9) which plays a role in tumorigenesis in cell cancer lines.

Biochem/physiol Actions

(R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.(S)-PFI-2, an enantiomer of (R)-PFI-2, is used as a negative control. (S)-PFI-2 is available from Sigma. To learn more about and purchase (S)-PFI-2, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

PFI-2 (hydrochloride) 준비 용품 및 원자재

원자재

준비 용품


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