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Cat. No. Product Name CAS No. Information
PC-61389

Nedisertib

1637542-33-6

Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK; sensitizes multiple tumor cell lines to radiation therapy in vitro and strongly enhances the antitumor activity of ionizing radiation in vivo.

Lung Cancer

Phase 2 Clinical

PC-43460

PIK-75

372196-77-5 PIK-75 is a potent, isoform-selective p110α inhibitor with IC50 of 0.3 nM, displays >100-fold selectivity over p110β, p110δ and PI3K C2b; blocks the phosphorylation of PKB induced by insulin on both Ser473 and Thr308 in CHO-IR cell (IC50=78 nM), inhibits PI3K activation associated with dramatic suppression of downstream signaling events, including AKT phosphorylation, IKK activation, and NF-kappaB transcription; potently and dose dependently inhibits in vitro and in vivo production of TNF-alpha and IL-6, diminishes the induced expression of human endothelial cell adhesion molecules (E-selectin, ICAM-1, and VCAM-1), and blocks human monocyte-endothelial cell adhesion; exhibits significant anti-tumor effectiveness in vivo.
PC-63031

KU-0060648

881375-00-4 KU-006064 is a potent, dual inhibitor of DNA-PK (IC50=8.6 nM) and PI3K (IC50=4/0.5/0.1 nM for PI3Kα/β/δ); shows selectively over other PI-3K-like kinases, such as ATM, ATR and mTOR; inhibits cellular DNA-PK autophosphorylation with IC50 of 19 nM (MCF7 cells) and 170 nM (SW620 cells); reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
PC-62996

IC 86621

404009-40-1 IC 86621 is a potent DNA-PK inhibitor with IC50 of 135 nM, also inhibits p110β (IC50=135 nM), less potent for p110α/γ/δ (IC50=880-1,400 nM); directly inhibits the repair of DNA DSBs and consequently enhances the cytotoxicity of physical and chemical agents that induce DSBs but not other DNA lesions.
PC-62995

IC 87361

404011-02-5 IC 87361 is a potent and selective DNA-PK inhibitor with IC50 of 34 nM, shows >50-fold selectivity over p110β; enhances radiation sensitivity in wild-type C57BL6 endothelial cells; induces radiosensitization of tumor microvasculature in wild-type mice.
PC-61971

VX-984

1562396-65-9 VX-984 (M 9831) is a potent, selective inhibitor of DNA-PK with IC50 of 88±64 nM for inhibition of DNA-PKcs autophosphorylation (Ser2056) in A549 lung cancer cells, with good selectivity versus other PI3K family members.

Solid Tumors

Phase 1 Clinical

PC-61970

SU-11752

688036-19-3 SU-11752 is a potent, selective inhibitor of DNA-PK, >500-fold selectivity over PI3Kγ, inhibits DNA double-strand break repair in cells and sensitizs ionizing radiation in cancer cells.

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