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SML1257

KU-0060648

Name: KU-0060648
Brand: SIGMA

≥98% (HPLC), DNA-PK and PI3K inhibitor, powder

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):

C₃₃H₃₄N₄O₄S

CAS Number:

881375-00-4

Molecular Weight:

582.71

UNSPSC Code:

12352200

PubChem Substance ID:

329825749

NACRES:

NA.77

MDL number:

MFCD17214218

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

KU-0060648, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 1 mg/mL, clear (warmed)

storage temp.

−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

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

Biochem/physiol Actions

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.

KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K.

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).

pictograms

GHS06

signalword

Danger

hcodes

H301

pcodes

P264 - P270 - P301 + P310 - P405 - P501

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

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

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Certificates of Analysis (COA)

Lot/Batch Number

0000425704

0000145875

0000114312

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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)

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)

Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.

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

PARP Inhibitor Olaparib Causes No Potentiation of the Bleomycin Effect in VERO Cells, Even in the Presence of Pooled ATM, DNA-PK, and LigIV Inhibitors.

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

Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.

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

Global Trade Item Number

SKU	GTIN
SML1257-5MG	04061832434742
SML1257-25MG	04061832434735

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