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DNA-PK

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-dependent protein kinase (9)
产品名称 目录号 简述
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)是DNA-PK选择性抑制剂,IC50为14 nM,对mTOR,PI3K,ATM和ATR的抑制性较弱。

LTURM34 HY-101667

LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.

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是DNA修复酶DNA-PK抑制剂,IC50为0.23 uM,对PIKK家族其它酶抑制性较弱。

PIK-75 HY-13281

PIK-75是p110α抑制剂,IC50为 5.8 nM,比对p110β的抑制性强200倍,还能抑制DNA-PK,IC50为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.

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