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AB120968

Compound 401, DNA-dependent protein kinase and mTOR inhibitor

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MW 281.31 Da, Purity >99%. 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.

View Alternative Names

DNA PK, DNA-PK catalytic subunit, DNA-PKcs, DNA-dependent protein kinase catalytic subunit, DNPK 1, FK506 binding protein 12 rapamycin associated protein 1, FK506 binding protein 12 rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, FLJ44809, FRAP, FRAP1, FRAP2, HYRC, HYRC 1, Hyper radiosensitivity of murine scid mutation, complementing 1, Hyperradiosensitivity complementing 1, mouse, homolog of 1, IMD26, MTOR_HUMAN, Mammalian target of rapamycin, Mechanistic target of rapamycin, OTTHUMP00000001983, PKRDC, PRKDC_HUMAN, Protein Kinase DNA Activated Catalytic Polypeptide, RAFT1, RAPT1, Rapamycin and FKBP12 target 1, Rapamycin associated protein FRAP2, Rapamycin target protein, Rapamycin target protein 1, Serine/threonine-protein kinase mTOR, XRCC 7, dJ576K7.1 (FK506 binding protein 12 rapamycin associated protein 1), p350, p460

1 Images
Chemical Structure - Compound 401, DNA-dependent protein kinase and mTOR inhibitor (AB120968)
  • Chemical Structure

Lab

Chemical Structure - Compound 401, DNA-dependent protein kinase and mTOR inhibitor (AB120968)

2D chemical structure image of ab120968, Compound 401, DNA-dependent protein kinase and mTOR inhibitor

Key facts

CAS number

168425-64-7

Purity

>99%

Form

Solid

form

Molecular weight

281.31 Da

Molecular formula

C<sub>1</sub><sub>6</sub>H<sub>1</sub><sub>5</sub>N<sub>3</sub>O<sub>2</sub>

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.

Product protocols

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