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SML1257

KU-0060648

≥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
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Product Name

KU-0060648, ≥98% (HPLC)

Quality Segment

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

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

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

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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