콘텐츠로 건너뛰기
Merck
모든 사진(1)

Key Documents

View All Documentation

SML1257

Sigma-Aldrich

KU-0060648

≥98% (HPLC)

동의어(들):

4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide, KU 0060648

로그인조직 및 계약 가격 보기
모든 사진(1)

About This Item

실험식(Hill 표기법):
C33H34N4O4S
CAS Number:
881375-00-4
Molecular Weight:
582.71
MDL number:
MFCD17214218
UNSPSC 코드:
12352200
PubChem Substance ID:
329825749
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

형태

powder

색상

white to light brown

solubility

DMSO: 1 mg/mL, clear (warmed)

저장 온도

−20°C

SMILES string

O=C(CN1CCN(CC)CC1)NC2=CC=C(C3=CC=CC4=C3OC(N5CCOCC5)=CC4=O)C6=C2C(C=CC=C7)=C7S6

InChI

1S/C33H34N4O4S/c1-2-35-12-14-36(15-13-35)21-29(39)34-26-11-10-23(33-31(26)25-6-3-4-9-28(25)42-33)22-7-5-8-24-27(38)20-30(41-32(22)24)37-16-18-40-19-17-37/h3-11,20H,2,12-19,21H2,1H3,(H,34,39)

InChI key

AATCBLYHOUOCTO-UHFFFAOYSA-N

생화학적/생리학적 작용

KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K. The IC50 values for inhibition of DNA-PK in MCF7 and SW620 cells are 19 and 170 nM, respectively. The compound KU-0060648 inhibits MCF7 PI3K activity with an IC50 of 39 nM, but is inactive against PI3K in SW620, suggesting a cell-dependent mechanism of inhibition. KU-0060648 increases sensitivity to DNA damaging cytotoxic drugs such as etoposide and doxorubicin in tumor cell lines expressing DNA-PK. KU-0060648 stimulates Cas9 (CRISPR associated protein 9) mediated genome editing by enhancing the rate of homology directed-repair (HDR) and decreasing the rate of NHEJ (non-homologous end-joining).
KU-0060648 is observed to inhibit proliferation and initiate apoptosis in hepatocellular carcinoma. KU-0060648 is useful in chemotherapy as it increases the efficiency of double stranded breaks initiated by anticancer drugs.

픽토그램

Skull and crossbones
GHS06

신호어

Danger

유해 및 위험 성명서

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.

이 제품을 이미 가지고 계십니까?

문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

Joanne M Munck et al.
Molecular cancer therapeutics, 11(8), 1789-1798 (2012-05-12)
DNA double-strand breaks (DSB) are the most cytotoxic lesions induced by topoisomerase II poisons. Nonhomologous end joining (NHEJ) is a major pathway for DSB repair and requires DNA-dependent protein kinase (DNA-PK) activity. DNA-PK catalytic subunit (DNA-PKcs) is structurally similar to
KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms.
Chen M B, et al.
Oncotarget, 7(13), 17047-17047 (2016)
Developments of DNA-dependent protein kinase inhibitors as anticancer agents.
Ma C C, et al.
Mini-Reviews in Medicinal Chemistry, 14(11), 884-895 (2014)
Valentina Perini et al.
International journal of molecular sciences, 21(21) (2020-11-11)
Poly(ADP-ribosyl)polymerase (PARP) synthesizes poly(ADP-ribose) (PAR), which is anchored to proteins. PAR facilitates multiprotein complexes' assembly. Nuclear PAR affects chromatin's structure and functions, including transcriptional regulation. In response to stress, particularly genotoxic stress, PARP activation facilitates DNA damage repair. The PARP
Francis Robert et al.
Genome medicine, 7, 93-93 (2015-08-27)
The ability to modify the genome of any cell at a precise location has drastically improved with the recent discovery and implementation of CRISPR/Cas9 editing technology. However, the capacity to introduce specific directed changes at given loci is hampered by

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

고객지원팀으로 연락바랍니다.