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Request The Product List ofATM/ATR ATM/ATR

     ATM/ATR are members of the PI3 family of serine-threonine kinases and function as essential links between the sensors and effectors of the DNA damage response. The roles of ATM and ATR partially overlap and are cooperative; however they are also known to play distinct roles in protecting the cell from DNA damage.


     ATM is mostly responsible for sending signals from DSBs (double-strand breaks) induced by ionizing radiation while the closely related ATR responds to UV damage or stalled replication forks. ATM and ATR are known to phosphorylate common as well as specific substrates to activate checkpoint signaling. The G1, S, and G2 cell cycle checkpoints are primarily regulated by the ATM (ataxia telangiectasia, mutated) and ATR (ATM and Rad3-related) protein kinases.

Cat. No. Product Name CAS No. Information
GY01983

BAY-1895344 hydrochloride

BAY-1895344 is a potent, selective, orally active ATR inhibitor with low-nanomolar potency; potently inhibits the proliferation of a broad spectrum of human tumor cell lines with mean IC50 of 78 nM; inhibits hydroxyurea-induced H2AX phosphorylation, exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models.

GY04116

GJ103 sodium salt

1459687-96-7

A novel small molecular read-through (SMRT) compound that can induce read through of nonsense mutations in the ATM gene; induces ATM kinase on both TGA and TAG stop codons and restores ATMpSer1981 autophosphorylation and SMC1pSer966 transphosphorylation in A-T cells.

GY05201

AZ-31

2088113-98-6

A potent, highly selective and orally active ATM inhibitor with enzyme IC50 of <1.2 nM, cell IC50 of 46 nM; displays excellent selectivity against a panel of kinases including ATR, DNAPK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, GSK3β and KDR; reduces upregulation of p21 and blocks G1 arrest in wild-type but not Cdkn1a(p21CIP/WAF1)-/- mice; showes significant tumor growth reduction in the SW620 xenograft model combined with irinotecan.

GY05106

CBP-93872

67427-51-4

A potent G2 checkpoint inhibitor that specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint; directly suppresses the growth of p53-mutated cancer cell lines with wild-type CDKN2A by eliciting G(1) arrest, but not CDKN2A-deleted and/or wild-type p53 lines; decreases phospho-cdc2 Y15 by inhibiting phosphorylation of Chk1; specifically inhibits DSB-mediated and Nbs1-dependent activation of ATR.

GY05055

GSK 635416A

944729-29-7

GSK 635416A is a novel ATM inhibitor with highly selective radiosensitizing activity, inhibits radiation induced phosphorylation of ATM; exhibits virtually no cytotoxicity in the absence of radiation and in normal fibroblast cells, enhances IR effect in radiosensitizing HNSCC cell lines but not in normal fibroblast BJ-ET cells in combined with olaparib.

GY04482

BAY 1895344

1876467-74-1

BAY-1895344 is a potent, selective, orally active ATR inhibitor with low-nanomolar potency; potently inhibits the proliferation of a broad spectrum of human tumor cell lines with mean IC50 of 78 nM; inhibits hydroxyurea-induced H2AX phosphorylation, exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models.

GY01751

CP-466722

1080622-86-1

CP-466722 is a poten and selective ATM inhibitor without effect on ATR kinase; does not inhibit PI3K, PI3K-like protein kinases or Abl kinase and disrupts ATM-dependent cell cycle checkpoints in cells.

GY01453

AZD-0156

1821428-35-6

AZD-0156 (AZD0156, AZD 0156) is a potent, highly selective and orally bioavailable ATM inhibitor; exhibits antitumoral activity, both reducing tumor burden and preventing tumors from growing in an immunocompetent allograft mouse model of AML.

GY01151

AZD-6738

1352226-88-0

AZD-6738 (AZD6738, Ceralasertib) is a potent and selective inhibitor of ATR with IC50 of 1 nM; shows no significant activity for ATM, DNA-PK and mTOR; inhibits ATR kinase-dependent CHK1 phosphorylation in cells (IC50=74 nM); enhances the therapeutic efficacy of cisplatin in xenograft models; orally active and bioavailable.

GY01100

VE-821

1232410-49-9

VE-821 is a potent, selective and ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM; shows excellent selectivity for ATR over the related PIKKs ATM, DNA-PK, mTOR and PI3K.

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