Drug Information

Drug General Information
Drug ID
D0R0TW
Former ID
DIB020148
Drug Name
KU-0060648
Synonyms
KU 0060648
Drug Type
Small molecular drug
Indication Discovery agent Investigative [531901]
Structure
Download
2D MOL
Formula
C33H34N4O4S
InChI
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)
InChIKey
AATCBLYHOUOCTO-UHFFFAOYSA-N
PubChem Compound ID
11964036
PubChem Substance ID
22422302, 26544618, 36461104, 78916591, 103759129, 104154287, 137275889, 137365723, 140801386, 177748923, 196375773, 226088041, 230069714, 241377205, 244797915, 249565691, 252158405, 252472226
Target and Pathway
Target(s) PI3K beta Target Info Inhibitor [532428]
DNA-dependent protein kinase catalytic subunit Target Info Inhibitor [532428]
Phosphoinositide 3 kinase Target Info Inhibitor [532428]
BioCyc Pathway Superpathway of inositol phosphate compounds
3-phosphoinositide biosynthesis
KEGG Pathway Inositol phosphate metabolism
ErbB signaling pathway
Ras signaling pathway
Rap1 signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
HIF-1 signaling pathway
FoxO signaling pathway
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK signaling pathway
Apoptosis
Adrenergic signaling in cardiomyocytes
VEGF signaling pathway
Osteoclast differentiation
Focal adhesion
Signaling pathways regulating pluripotency of stem cells
Platelet activation
Toll-like receptor signaling pathway
Jak-STAT signaling pathway
Natural killer cell mediated cytotoxicity
T cell receptor signaling pathway
B cell receptor signaling pathway
Fc epsilon RI signaling pathway
Fc gamma R-mediated phagocytosis
TNF signaling pathway
Leukocyte transendothelial migration
Neurotrophin signaling pathway
Cholinergic synapse
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Regulation of lipolysis in adipocytes
Type II diabetes mellitus
Non-alcoholic fatty liver disease (NAFLD)
Aldosterone-regulated sodium reabsorption
Carbohydrate digestion and absorption
Bacterial invasion of epithelial cells
Chagas disease (American trypanosomiasis)
Toxoplasmosis
Amoebiasis
Hepatitis C
Hepatitis B
Measles
Influenza A
HTLV-I infection
Epstein-Barr virus infection
Pathways in cancer
Viral carcinogenesis
Proteoglycans in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Melanoma
Chronic myeloid leukemia
Acute myeloid leukemia
Small cell lung cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
Choline metabolism in cancerhsa03450:Non-homologous end-joining
Cell cyclehsa00562:Inositol phosphate metabolism
MicroRNAs in cancer
Choline metabolism in cancer
NetPath Pathway IL1 Signaling Pathway
PANTHER Pathway Angiogenesis
Apoptosis signaling pathway
Axon guidance mediated by netrin
B cell activation
EGF receptor signaling pathway
Endothelin signaling pathway
FGF signaling pathway
Hypoxia response via HIF activation
Inflammation mediated by chemokine and cytokine signaling pathway
Insulin/IGF pathway-protein kinase B signaling cascade
Integrin signalling pathway
Interleukin signaling pathway
PDGF signaling pathway
PI3 kinase pathway
T cell activation
VEGF signaling pathway
p53 pathway
Ras Pathway
p53 pathway feedback loops 2
CCKR signaling map ST
Pathway Interaction Database ErbB4 signaling events
LPA receptor mediated events
TRAIL signaling pathway
Signaling events mediated by TCPTP
FAS (CD95) signaling pathway
CXCR4-mediated signaling events
EGF receptor (ErbB1) signaling pathway
Class I PI3K signaling events
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
PDGFR-beta signaling pathway
Nephrin/Neph1 signaling in the kidney podocyte
Internalization of ErbB1
CXCR3-mediated signaling eventsdnapk_pathway:DNA-PK pathway in nonhomologous end joining
Coregulation of Androgen receptor activity
Class I PI3K signaling events mediated by Akt
BARD1 signaling events
PathWhiz Pathway Inositol Metabolism
Phosphatidylinositol Phosphate Metabolism
Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Fc Epsilon Receptor I Signaling in Mast Cells
Reactome PI3K Cascade
GPVI-mediated activation cascade
PIP3 activates AKT signaling
PI3K/AKT activation
Role of phospholipids in phagocytosis
Tie2 Signaling
Constitutive Signaling by Aberrant PI3K in Cancer
DAP12 signaling
Role of LAT2/NTAL/LAB on calcium mobilization
Nephrin interactions
G beta:gamma signalling through PI3Kgamma
VEGFA-VEGFR2 Pathway
Interleukin-3, 5 and GM-CSF signaling
Interleukin receptor SHC signaling
Regulation of signaling by CBLR-HSA-5693571:Nonhomologous End-Joining (NHEJ)R-HSA-109704:PI3K Cascade
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
PI3K events in ERBB4 signaling
GAB1 signalosome
PI3K events in ERBB2 signaling
Costimulation by the CD28 family
CD28 dependent PI3K/Akt signaling
G alpha (q) signalling events
G alpha (12/13) signalling events
Constitutive Signaling by EGFRvIII
PI-3K cascade:FGFR1
PI-3K cascade:FGFR2
PI-3K cascade:FGFR3
PI-3K cascade:FGFR4
Regulation of signaling by CBL
WikiPathways Toll-like receptor signaling pathway
DNA Damage Response (only ATM dependent)
G13 Signaling Pathway
Regulation of Actin Cytoskeleton
Insulin Signaling
Fc epsilon receptor (FCERI) signaling
PI Metabolism
Interleukin-2 signaling
Fcgamma receptor (FCGR) dependent phagocytosis
DAP12 interactions
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
PIP3 activates AKT signaling
Signaling Pathways in Glioblastoma
TCR signaling
Signaling by PDGF
Signaling by Insulin receptor
NGF signalling via TRKA from the plasma membrane
Nephrin interactions
Interleukin-3, 5 and GM-CSF signaling
GPVI-mediated activation cascade
Cell surface interactions at the vascular wall
MicroRNAs in cardiomyocyte hypertrophy
Regulation of toll-like receptor signaling pathway
AMPK SignalingWP707:DNA Damage Response
Non-homologous end joining
FAS pathway and Stress induction of HSP regulation
Cytosolic sensors of pathogen-associated DNA
Retinoblastoma (RB) in Cancer
Prostate Cancer
Double-Strand Break Repair
Cell Cycle
miRNA Regulation of DNA Damage ResponseWP75:Toll-like receptor signaling pathway
Serotonin HTR1 Group and FOS Pathway
IL-4 Signaling Pathway
Copper homeostasis
Signaling of Hepatocyte Growth Factor Receptor
Transcriptional activation by NRF2
IL1 and megakaryotyces in obesity
Signaling by ERBB4
Signaling by ERBB2
Signaling by SCF-KIT
Gastrin-CREB signalling pathway via PKC and MAPK
Integrated Pancreatic Cancer Pathway
TSLP Signaling Pathway
Regulation of Microtubule Cytoskeleton
TSH signaling pathway
SREBP signalling
Signaling by FGFR
Signaling by EGFR
GPCR downstream signaling
Costimulation by the CD28 family
Angiogenesis
AMPK Signaling
References
Ref 531901Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol Cancer Ther. 2012 Aug;11(8):1789-98.
Ref 5324281-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.

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