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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 |
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| AZD7762
AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively. |
| BIBR1532
BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. |
| PF-477736
PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively. |
| SCH 900776
SCH 900776 (MK-8776) is a highly potent and functionally selective CHK1 inhibitor with IC50 of 3 nM. |
| Rabusertib (LY2603618)
Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM. |
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