| DC70085 |
Nedisertib (Synonyms: Peposertib; M3814)
|
Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK. |
| DC46491 |
BAY-8400
|
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 81 nM. BAY-8400 shows synergistic activity of DNA-PK inhibition when combined with DNA damage inducing cancer therapy, like targeted alpha radiation. |
| DC3113 |
KU-0060648
|
KU 0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. |
| DC73198 |
ZL-2201 mesylate
|
ZL-2201 mesylate (ZL2201) is a highly potent, selective and orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 1.1 nM. |
| DC73197 |
SN38023
|
SN38023 is a bioreductive prodrug of DNA-dependent protein kinase inhibitor IC87361 (Cat# PC-62995), SN38023 is metabolised to a potent DNA-PKi (IC87361) selectively in radioresistant hypoxic cells. |
| DC73196 |
Ku-DBi 245
|
Ku-DBi 245 is a novel DNA-PK inhibitor with a unique mechanism of action, blocking the Ku 70/80 heterodimer interaction with DNA. |
| DC72318 |
Canfosfamide
|
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies. |
| DC70667 |
NU5455
|
NU5455 (NU-5455) is a potent, highly selective, oral inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs) activity with IC50 of 8.2 nM.NU5455 displays selectivity versus Vps34 (8.7-fold), PI3Kδ (33.7-fold), ATM/ATR (both >1200-fold), 228-fold selectivity margin for DNA-PKcs kinase activity versus that of PI3Kα.NU5455 inhibited radiation-induced activation of DNA-PK with an IC50 of 168 nM, but did not inhibit IGF-stimulated activation of AKT in MCF7 cells even at 10 uM.NU5455 inhibited the repair of DNA-DSBs induced by treatment with enzyme AfeI or ScaI restriction endonucleases within a 24-hour period in HEK293T cells, significantly increased the number of colocalized γH2AX and 53BP1 foci.NU5455 is a highly selective inhibitor of DNA-PKcs that is active in cells and that can perturb DNA-DSB repair by NHEJ.NU5455 preferentially augmented radiotherapy in subcutaneous Calu-6 and A549 lung tumor xenografts, increased both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor, NU5455 enhanced the activity of doxorubicin released locally in liver tumor xenografts without inducing any adverse effect. |
| DC49559 |
DNA-PK-IN-3
|
DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4). |
| DC49558 |
DNA-PK-IN-4
|
DNA-PK-IN-4 is a potent inhibitor of DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27). |
