atm/atr

Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride.

Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitizer for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest. Ro 90-7501 also exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.

Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.

ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.

VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki IC50: 13 26 nM in cell-free assays).

GJ103 sodium salt is an active analog of GJ072, a read-through compound. It has been shown to reduce the surface tension of aqueous solutions, which makes it easier for molecules to move through the solution. It has also been shown to reduce the viscosity of aqueous solutions, which makes it easier for molecules to move through the solution. Additionally, it has been shown to reduce the pH of aqueous solutions, which can have a variety of effects on the biochemical and physiological processes of living organisms.

Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.

Elimusertib hydrochloride(1876467-74-1 free base) (BAY-1895344 hydrochloride) is a effective, orally available and selective ATR inhibitor with anti-tumor activity.

AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.

AD1058 is a potent and selective ATR inhibitor (IC50 = 1.6 nM) that crosses the blood-brain barrier with significant in vivo anticancer activity. It is commonly used in the study of brain metastasis and CNS metastasis by inhibiting cell proliferation, disrupting the cell cycle and inducing apoptosis.

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.

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

Berzosertib (VE-822) is an ATR inhibitor (Ki<0.2 nM) that also inhibits ATM (Ki=34 nM). Berzosertib has antitumor activity and has been used in trials investigating the treatment of ovarian tumors, plasmacytoid tumors of the ovary, solid tumors in adults, advanced solid tumors, and advanced solid tumors.

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.

Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC50 of 1 nM.

AZD1390 is an exceptionally potent inhibitor of ATM in cells (IC50: 0.78 nM) with >10,000-fold selectivity over closely related members of the PIKK family of enzymes.

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.

Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.

CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.

Lartesertib (ATM Inhibitor-5) is an inhibitor of serine/threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.

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.

KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).

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.