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KU-0060648

SIGMA/SML1257 - ≥98% (HPLC)

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

CAS Number: 881375-00-4
Empirical Formula (Hill Notation): C33H34N4O4S
Molecular Weight: 582.71
MDL Number: MFCD17214218
Linear Formula: C33H34N4O4S
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML1257-5MG 5 mg
 $178.00
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45-SML1257-25MG 25 mg
 $712.00
1/EA		 Add To Favorites

 

assay ≥98% (HPLC)
color white to light brown
form powder
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
Quality Level 100 
SMILES string O=C(CN1CCN(CC)CC1)NC2=CC=C(C3=CC=CC4=C3OC(N5CCOCC5)=CC4=O)C6=C2C(C=CC=C7)=C7S6
solubility DMSO: 1 mg/mL, clear (warmed)
storage temp. −20°C
Biochem/physiol Actions: KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K.
Biochem/physiol Actions: 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).
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.
Packaging: 5, 25 mg in glass bottle
Purity ≥98% (HPLC)
Storage Temp. −20°C
UNSPSC 12352200

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