Signaling Pathway

DNA-PK

DNA-PK

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DNA-PKcs (DNA-dependent protein kinase, catalytic subunit) is an enzyme that in humans is encoded by the PRKDC gene. DNA-PKcs belongs to the phosphatidylinositol 3-kinase-related kinase protein family. DNA-PKcs is the catalytic subunit of a nuclear DNA-dependent serine/threonine protein kinase called DNA-PK. The second component is the autoimmune antigen Ku. On its own, DNA-PKcs is inactive and relies on Ku to direct it to DNA ends and trigger its kinase activity. DNA-PKcs is required for the non-homologous end joining (NHEJ) pathway of DNA repair. Many proteins have been identified as substrates for the kinase activity of DNA-PK. Autophosphorylation of DNA-PKcs appears to play a key role in NHEJ and is thought to induce a conformational change that allows end processing enzymes to access the ends of the double-strand break. DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNA damage checkpoint.

DNA-PK Inhibitors & Modulators (8)

Product Name Catalog No. Brief Description
CC-115

HY-16962

CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

CC-115 hydrochloride

HY-16962A

CC-115 hydrochloride is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

Compound 401

HY-19341

Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K.

KU-57788

HY-11006

KU-57788(NU7441) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 value of  are 14 nM; 1700, 5000, >100000 and >100000 nM for  mTOR, PI 3K, ATM and ATR respectively; also is a modest inhibitor of BRD4 and BRDT with IC50s of 1 and 3.5 uM respectively.

LY3023414

HY-12513

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).

NU 7026

HY-15719

NU 7026 is a novel and potential inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK) with IC50 of 0.23 uM; displays selectivity over other PIKK family enzymes.

PIK-75

HY-13281

PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.

Wortmannin

HY-10197

Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50 of 3 nM and 0.17 μM, respectively.