DNA-PK
The DNA-PK holoenzyme comprises a heterodimer of approximately 70- and 80-kDa polypeptides, known as Ku, that binds to DNA strand breaks, recruiting and activating the 470-kDa catalytic subunit, termed DNA-PKcs. Cells lacking DNA-PK are hypersensitive to IR and cross-linking agents and defective in DSB repair. DNA-PK, together with the x-ray cross complementing (XRCC4)/DNA ligase IV complex and the recently identified cofactor Artemis, is specifically required for NHEJ, with about 80% of DNA DSBs repaired by this pathway. DNA-PK can accelerate the repair of IR-, etoposide-, and doxorubicin-induced DSBs, thus conferring resistance to these agents. The inhibition of DNA-PK is an attractive approach for modulating resistance to therapeutically-induced DNA DSBs.
References
1.Furgason JM,et al. Pharmacol Ther. 2013;137(3):298–308.
References
1.Furgason JM,et al. Pharmacol Ther. 2013;137(3):298–308.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
DNA-PK
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VX-984 B
产品货号 : M32889
cas no: 1476074-39-1
VX-984 是一种口服有效、选择性的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 有效抑制 NHEJ (非同源性末端接合),增加DSBs (DNA 双链断裂)。VX-984 可用于胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSCLC) 的研究。VX-984 是一种从头设计的氘代物。 -
ETP-45658
产品货号 : M27815
cas no: 1198357-79-7
ETP 45658 是一种 PI 3-激酶抑制剂(PI 3-Kα、PI 3-Kδ、PI 3-Kβ 和 PI 3-Kγ 的 IC50 值分别为 22、30、129 和 710 nM)。 -
STL127705
产品货号 : M26468
cas no: 1326852-06-5
STL127705 是一种有效的 Ku 70/80 异二聚体蛋白抑制剂,可抑制 Ku70/80-DNA 相互作用,IC50 为 3.5 μM。 STL127705 抑制 Ku 依赖性 DNA-PKCS 激酶的激活,IC50 为 2.5 μM。 -
AZD-7648
产品货号 : M20665
cas no: 2230820-11-6
AZD-7648 是一种 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂,酶测定中 IC50 为 0.63 nM,具有抗肿瘤活性。 -
Caudatin
产品货号 : M18501
cas no: 38395-02-7
Caudatin 是主要从 Cynanchum bungei Decne 根中分离出来的 C-21 甾体糖苷之一,具有有效的抗癌活性。