| Cat. No. |
Product Name |
CAS No. |
Information |
| H9473 |
Gartisertib
|
1613191-99-3 |
Gartisertib(VX-803) is an orally available inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase, with potential antineoplastic activity. |
| H1848 |
VE-821
|
1232410-49-9 |
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. |
| H1847 |
KU-60019
|
925701-46-8 |
KU-60019 is an improved analogue of KU-55933, and is a potent, specific inhibitor of ATM kinase with IC50 of 6.3 nM, 270- and 1,600-fold selectivity over DNA-PKcs and ATR; blocks radiation-induced phosphorylation of key ATM targets in human glioma cells, which is 10-fold more effective than KU-55933, reduces basal S473 AKT phosphorylation and inhibits glioma cell migration and invasion in vitro; preferentially sensitizes p53-mutant glioma to ionizing radiation in orthotopic xenograft models of GBM. |
| H1846 |
KU-55933
|
587871-26-9 |
KU-55933 is a potent, specific, ATP-competitive inhibitor of ATM with Ki/IC50 of 2.2/13 nM, >100-fold selectivity against other members of the PIKK family kinases; inhibits ATM-dependent p53 Ser15 phosphorylation in U2OS osteosarcoma cells with IC50 of 0.3 uM, sensitizes the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents, etoposide, doxorubicin, and camptothecin; also suppresses the replication of both wild-type and drug-resistant HIV-1 by sensitizing cells to retrovirus-induced cell death. |
| H1845 |
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. |
| H1844 |
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. |
| H1843 |
CP-466722
|
1080622-86-1 |
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. |
| H1842 |
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. |
| H1841 |
BAY-1895344 hydrochloride
|
|
Elimusertib(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. |
| H1840 |
BAY-1895344
|
1876467-74-1 |
BAY-1895344(Elimusertib) 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. |
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