UCN-01

UCN-01 구조식 이미지
카스 번호:
112953-11-4
상품명:
UCN-01
동의어(영문):
UNC 01;UCN-01;KW-2401;KRX-0601;NSC 638850;UCN01,UCN 01;KRX-0601,UCN-01;7-hydroxystaurosporine;(5S,6R,7R,9R,16R)-16-Hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-17-oxa;(9S)-2,3,10,11,12,13-Hexahydro-3α-hydroxy-10α-methoxy-9-methyl-11α-methylamino-9β,13β-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one
CBNumber:
CB2972499
분자식:
C28H26N4O4
포뮬러 무게:
482.53044
MOL 파일:
112953-11-4.mol
MSDS 파일:
SDS

UCN-01 속성

끓는 점
705.7±60.0 °C(Predicted)
밀도
1.63±0.1 g/cm3(Predicted)
저장 조건
2-8°C
용해도
에 용해됨 DMSO: >5mg/mL
물리적 상태
황갈색 고체
산도 계수 (pKa)
12.25±0.70(Predicted)
색상
연노랑
optical activity
[α]20/D 130 to 160°, c = 0.2 in DMSO

안전

WGK 독일 3
RTECS 번호 KC6600010
독성 mouse,LD50,intraperitoneal,25mg/kg (25mg/kg),Journal of Antibiotics. Vol. 42, Pg. 571, 1989.

UCN-01 C화학적 특성, 용도, 생산

개요

UCN-01 is a synthetic derivative of staurosporine with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM) and cyclin-dependent kinases (IC50s = 300-600 nM for Cdk1 and Cdk2). UCN-01 arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase Chk1 (IC50 = 7 nM), leading to apoptosis.

용도

UCN-01 is an indolocarbazole isolated from a high staurosporine-producing Streptomyces culture. UCN-01 inhibits protein kinase C (PKC) and cyclin-dependant kinase 2 (CDK2), resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by the latter agents.

일반 설명

A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC50 = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC50 = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC50 = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents.

UCN-01 준비 용품 및 원자재

원자재

준비 용품


UCN-01 공급 업체

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Career Henan Chemica Co
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BOC Sciences 1-631-485-4226; 16314854226
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Shanghai Aladdin Bio-Chem Technology Co.,LTD 400-6206333 18521732826;
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ShangHai Caerulum Pharma Discovery Co., Ltd. 18149758185
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