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CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM. CCT241533 hydrochloride shows minimal cross-reactivity against a panel of kinases at 1 uM. CCT241533 HCl blocked CHK2 activity in human tumor cell lines in response to DNA damage, as shown by inhibition of CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. CCT241533 did not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. CCT241533 HCl abolished the induction of the pS516 CHK2 signal, implying that the potentiation of PARP inhibitor cell killing by CCT241533 was due to inhibition of CHK2.
| Molecular Weight | 478.94 |
| Formula | C23H27FN4O4.HCl |
| CAS Number | 1431697-96-9 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
|---|
| PV-1019
PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits IR-induced apoptosis. |
| CCT241533 dihydrochloride
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM. |
| CBP501 Affinity Peptide
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. |
| Chktide
Chktide is a substrate for CHK1 and CHK2. |
| Zn-DPA-maytansinoid conjugate 1
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. |
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