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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 是一种有效的,选择性的 DNA-PK 抑制剂,并且适度抑制 BRD4BRDTIC50 值分别为 13 nM,1 μM 和 3.5 μM;同时能够激活 CRISPR/Cas9

LTURM34 HY-101667

LTURM34是DNA-PK的特异抑制剂,IC50值为0.034 μM。

LY3023414 HY-12513

LY3023414 是一种新颖的,可溶的 PI3KmTORDNA-PK 抑制剂。

NU 7026 HY-15719

NU 7026 是一种新型特异性的 DNA-PK 抑制剂,IC50 为 0.23±0.01 μM,也抑制 PI3KIC50 为 13±3 μM。

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 是一种多靶点抑制剂,能够抑制 PI3KMLCK 的活性,IC50 值分别为 3 nM 和 170 nM。

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