Abcam, ab120968, Compound 401, DNA-dependent protein kinase and mTOR inhibitor

Size: 10mg / 50mg
MW 281.31 Da, Purity >99%. Selective, reversible DNA-dependent protein kinase and mTOR inhibitor (IC 50 values are 0.28 and 5.3 μM respectively). No affinity for PI3K, ATM and ATR (IC 50 values are >100 μM). Able to induce apoptosis in vitro . Cell-permeable.
Key facts
CAS number:168425-64-7,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:281.31 Da,
Molecular formula:C16H15N3O2,
PubChem:10039361,
Nature:Synthetic,
Solubility:Soluble in DMSO to 10 mM,
Biochemical name:2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one,
Biological description:Selective, reversible DNA-dependent protein kinase and mTOR inhibitor (IC50 values are 0.28 and 5.3 μM respectively). No affinity for PI3K, ATM and ATR (IC50 values are >100 μM). Able to induce apoptosis in vitro. Cell-permeable.,
Canonical smiles:C1COCCN1C2=CC(=O)N3C=CC4=CC=CC=C4C3=N2,
InChi:InChI=1S/C16H15N3O2/c20-15-11-14(18-7-9-21-10-8-18)17-16-13-4-2-1-3-12(13)5-6-19(15)16/h1-6,11H,7-10H2,
InChiKey:BVRDQVRQVGRNHG-UHFFFAOYSA-N,
IUPAC Name:2-morpholin-4-ylpyrimido[2,1-a]isoquinolin-4-one

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
DNA-PKcs (DNA-dependent protein kinase catalytic subunit) and mTOR (mechanistic Target of Rapamycin) are two important proteins with distinct roles. DNA-PKcs also known as PRKDC is a DNA repair protein with a molecular mass of approximately 469 kDa. It is part of the DNA-PK complex expressed mainly in the nucleus and high in tissues like the brain liver and spleen. mTOR is a pivotal protein kinase with a mass of about 289 kDa found widely throughout the body particularly in cells with high energy demands.
Biological function summary
DNA-PKcs functions in the repair of DNA double-strand breaks by facilitating non-homologous end joining (NHEJ). It forms a complex with Ku70/Ku80 proteins to recognize DNA damage. On the other side mTOR acts as a central regulator of cell growth and metabolism integrating signals from nutrients growth factors and energy conditions. mTOR is part of two distinct complexes mTORC1 and mTORC2. Both proteins ensure proper functioning of cellular processes by responding to DNA damage and energy availability respectively.
Pathways
DNA-PKcs plays a critical role in the DNA damage response pathway. It collaborates with other repair proteins including ATM and ATR to maintain genomic stability. mTOR involved in the PI3K/AKT/mTOR pathway regulates cell growth and survival by interacting with PDK1 and AKT proteins. These pathways are vital for cell cycle progression and survival under stress highlighting the integration of DNA repair mechanisms and metabolic control.
Both DNA-PKcs and mTOR are closely linked to cancer development. DNA-PKcs mutations can impair DNA repair leading to increased susceptibility to cancer due to genomic instability. mTOR deregulation is often seen in various cancers such as breast and prostate cancer due to its role in cell growth. DNA-PKcs can affect cancer progression through its interaction with tumor suppressor proteins like p53 while mTOR connects with proteins like PTEN and RHEB which modulate tumorigenic signaling pathways.