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ATM/ATR

ATM serine/threonine kinase, symbol ATM, is a serine/threonine protein kinase that is recruited and activated by DNA double-strand breaks. It phosphorylates several key proteins that initiate activation of the DNA damage checkpoint, leading to cell cycle arrest, DNA repair or apoptosis. Several of these targets, including p53, CHK2, BRCA1, NBS1 and H2AX are tumor suppressors. ATR is a serine/threonine kinase and belongs to the phosphoinositide 3- kinase related protein kinases (PIKKs), particularly to ATM (ataxia telangiectasia mutated) subfamily. It functions to maintain genome integrity by stabilizing replication forks and by regulating cell cycle progression and DNA repair.

Ceralasertib
T33381352226-88-0
Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC50 of 1 nM.
  • $43
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TargetMol | Inhibitor Hot
Elimusertib
T73181876467-74-1
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.
  • $31
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TargetMol | Inhibitor Hot
Elimusertib hydrochloride(1876467-74-1 free base)
T10468
Elimusertib hydrochloride(1876467-74-1 free base) (BAY-1895344 hydrochloride) is a effective, orally available and selective ATR inhibitor with anti-tumor activity.
  • $31
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ku-60019
T63872925701-46-8
KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).
  • $48
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Gartisertib
T104071613191-99-3In house
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
  • $136
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Wortmannin
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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Berzosertib
T26691232416-25-9
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.
  • $30
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azd1390
T51752089288-03-7
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.
  • $80
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KU-55933
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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torin 2
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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TargetMol | Inhibitor Sale
Camonsertib
T620832417489-10-0
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.
  • $172
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M3541
T708731360628-91-6
M3541 is a selectively potent and orally active ATM inhibitor with potential antitumor activity.M-3541 inhibits ATM kinase activity and ATM-mediated signaling by binding to ATM.M3541 prevents activation of DNA damage checkpoints, inhibits DNA damage repair, contributes to apoptosis, and induces death of ATM overexpressing tumor cells.
  • $518
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KU60019
T2474925701-49-1In house
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.
  • $48
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Tuvusertib
T104061613200-51-3
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.
  • $68
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Schisandrin B
T292561281-37-6
Schisandrin B (Schisandrin B (Sch B)) has an antioxidant effect on rodent liver and heart.
  • $35
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AZD0156
T67701821428-35-6
AZD0156 , an effective and specific inhibitors of ATM kinase, is potential antineoplastic activities and chemo- radio-sensitizing.
  • $31
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Garcinone C
TN167376996-27-5
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.
  • $38
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Dactolisib
T2235915019-65-7
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.
  • $39
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VE-821
T30321232410-49-9
VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki IC50: 13 26 nM in cell-free assays).
  • $30
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Lartesertib
T626842495096-26-7
Lartesertib (ATM Inhibitor-5) is an inhibitor of serine threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.
  • $132
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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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Ro 90-7501
T16773293762-45-5In house
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.
  • $30
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AD1058
T2001052907782-78-7
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.
  • $71
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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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