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DNA Damage/DNA Repair Filter
DNA Damage/DNA RepairDNA-PK
The DNA-dependent protein kinase (DNA-PK) is a serine/threonine protein kinase consisting of a catalytic subunit (DNA-PKcs) and a Ku heterodimer that is made up of the Ku70 and Ku80 subunits. DNA-PK was accidentally discovered after researchers studying translation found that double-stranded DNA (dsDNA) contaminated their preparations, leading to the phosphorylation of specific proteins.
Nedisertib
Cited
TQ00311637542-33-6
Nedisertib (M3814) is a specific inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 value less than 3 nM.
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CitedLY294002 Cited
T2008154447-36-6
LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5 0.57 0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.
- $34
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CitedWortmannin Cited
T628319545-26-7
Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.
- $40
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CitedPIK-75 Cited
T2667372196-67-3
PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
- $38
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CitedSTL127705
T130171326852-06-5In house
STL127705 (Compound L) is a potent inhibitor of the Ku 70 80 heterodimer protein, disrupting Ku70 80-DNA interaction with an IC50 of 3.5 μM, and inhibiting Ku-dependent DNA-PKCS kinase activation with an IC50 of 2.5 μM.
- $116
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AZD-7648
T71222230820-11-6
AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.
- $34
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Torin 1 Cited
T60451222998-36-8
Torin 1 is an effective inhibitor of mTORC1 2 with (IC50: 2 nM 10 nM); has 1000-fold selectivity for mTOR than PI3K.
- $30
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CitedAZD 6482
T60871173900-33-8
AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss.
- $31
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KU-57788
Cited
T6276503468-95-9
NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
- $34
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CitedTorin 2 Cited
T61001223001-51-1
Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.
- $35
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CitedVX-984
T110671476074-39-1
VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.
- $180
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Samotolisib
T68831386874-06-1
Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
- $41
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KU-55933 Cited
T2685587871-26-9
KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.
- $43
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CitedPIK-90
T2461677338-12-4
PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
- $39
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PI-103
T6143371935-74-9
PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2 3 3 15 30 23 nM for p110α β δ γ, mTOR, and DNA-PK).
- $52
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NU 7026
T2433154447-35-5
NU 7026 (DNA-PK Inhibitor II) is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR.
- $33
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PI3K-IN-1
T18261349796-36-6
PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.
- $30
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SF2523
T39861174428-47-7
SF2523 is a highly selective and potent inhibitor (SF2523) with improved physicochemical properties, excellent aqueous solubility, and biological efficacy. It is typically used in genome editing [CRISPR Cas Solution] technology and can effectively enhance the efficiency of this process.
- $31
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Leniolisib
T51661354690-24-6
Leniolisib (CDZ173) (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
- $72
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Onatasertib
T33511228013-30-6
Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).
- $35
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NU6027
T6612220036-08-8
NU6027 is a potent ATR CDK inhibitor, inhibits CDK1 2, ATR and DNA-PK with Ki of 2.5 μM 1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
- $37
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BAY-8400
T9498
BAY-8400 is a potent, selective, and orally active DNA-dependent protein kinase (DNA-PK) inhibitor (IC50 = 81 nM) that demonstrates synergistic efficacy when combined with targeted alpha therapies. BAY-8400 is applicable for cancer research [1].
- $77
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Voxtalisib
T7014934493-76-2
Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1 2.
- $32
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KU-0060648
T6557881375-00-4
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM.
- $54
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OSI-027 Cited
T6319936890-98-1
OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
- $35
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CitedPIK-75 hydrochloride
T2287372196-77-5
PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
- $36
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PI-3065
T2083955977-50-1
PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
- $44
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Pictilisib dimethanesulfonate
T11381957054-33-0
Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
- $30
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ETP-45658
T253991198357-79-7
ETP-45658 (ETP45658) is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively).
- $48
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ETP-46464 Cited
T20841345675-02-6
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
- $34
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CitedYU238259
T43391943733-16-1
YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.
- $40
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IC 86621
T9760404009-40-1
IC 86621 is a selective and reversible ATP-competitive inhibitor of DNA-PK with an IC50 of 120 nM. IC 86621 increases DNA double-strand break(DSB)-induced antitumor activity with an EC50 of 68 µM for DNA-PK mediated cellular DSB repair.
- $32
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Pilaralisib analogue
T2377956958-53-5
Pilaralisib analogue (XL147 analogue) is a selective and reversible class I PI3K inhibitor targeting PI3Kα δ γ.
- $32
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Compound 401
T3586168425-64-7
Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K.
- $29
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PIK-93
T2616593960-11-3
PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.
- $37
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(R)-(-)-Rolipram
T1344885416-75-7
(R)-(-)-Rolipram ((-)-Rolipram) is an R-enantiomer of Rolipram which is a PDE4 inhibitor.
- $39
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DMNB
T863720357-25-9
DMNB (6-Nitroveratraldehyde) is DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 15 μM, an enzyme involved in the non-homologous end-joining (NHEJ) pathway of double-stranded DNA break (DSB) repair in human cells.
- $29
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LTURM34
T157891879887-96-3
LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM. LTURM34 displays effective antiproliferative activity in a wide range of tumor cell lines. LTURM34 shows 170-fold selectivity for DNA-PK over PI3K .
- $38
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DNA-PK-IN-15
T2011602663852-17-1
DNA-PK-IN-15 (compound 6) acts as an inhibitor of DNA-PK, exhibiting an IC50 value of 0.08 nM.
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(Rac)-Nedisertib
T126721637542-34-7
(Rac)-Nedisertib is a racemate of Nedisertib, a potent inhibitor of DNA-PK(IC50 of <3 nM).
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ZL-2201
T786452865115-39-3
ZL-2201 is a potent inhibitor of DNA-PK, demonstrating an IC50 value of 1 nM.
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DNA-PK-IN-10
T791652919315-89-0
DNA-PK-IN-10 is a DNA-PK inhibitor used in breast cancer and non-small cell lung cancer research [1].
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