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SB 218078 is a inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging, enhancing the efficacy of some chemotherapeutics.
| Molecular Weight | 393.39 |
| Formula | C24H15N3O3 |
| CAS Number | 135897-06-2 |
| Solubility (25°C) | DMSO 39 mg/mL |
| 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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