ataxia-telangiectasia

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

Triheptanoin (IND 106011) is a fatty acid metabolic modulator. It potentially for the treatment of fatty acid oxidation disorders and GLUT1.

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

AZ32 is an orally bioavailable, blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for the ATM enzyme and an IC50 of 0.31 μM for ATM in cells.

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.

AZD0156 , an effective and specific inhibitors of ATM kinase, is potential antineoplastic activities and chemo-/radio-sensitizing.

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.

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

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

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

CGK733 (CGK 733) is a potent and selective inhibitor of ATM/ATR.

Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiectasia mutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031

ATR-IN-9 is a highly effective inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR). With an IC50 value as low as 10 nM, ATR-IN-9 demonstrates exceptional potency.

PROTAC ATR degrader-1 (compound ZS-7) serves as a powerful PROTAC degrader targeting ataxia telangiectasia and Rad3-related (ATR), exhibiting a DC50 of 0.53 μM. This compound is significant in the field of cancer research [1].

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.

ATR-IN-4, a potent inhibitor of ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.

Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.

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.

Ceralasertib is an orally available inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase. Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents 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.

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.

ART0380, a potent and selective ATR kinase inhibitor, exhibits specific antitumor activity for the research of Ataxia-Telangiectasia Mutated (ATM) aberrant cancers [1].

A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle arrest when combined with CPT-11, displaying notable antitumor activity [1].

Garcinone C is a xanthone derivative extracted from Garcinia oblongifolia Champ with anti-inflammatory, astringency, and granulation-promoting activities. Garcinone C is an AChE inhibitor and has potential cytotoxic effects on certain cancers.