135897-06-2
135897-06-2 structure
- Name: SB218078
- Chemical Name: sb 218078
- CAS Number: 135897-06-2
- Molecular Formula: C24H15N3O3
- Molecular Weight: 393.39400
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2017-09-30 07:07:28
- Modify Date: 2024-01-11 20:34:15
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SB-218078 is a potent, selective and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3].
| Name | sb 218078 |
|---|---|
| Synonyms |
hms3229o08
SB218078 |
| Description | SB-218078 is a potent, selective and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
Chk1:15 nM (IC50) Cdc2:250 nM (IC50) PKC:1000 nM (IC50) |
| In Vitro | SB-218078 (2.5-5 μM; 18 hours; HeLa cells) treatment abrogates G2 cell cycle arrest caused by either γ-irradiation or a topoisomerase I Topotecan inhibition[1]. SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage [1]. Cell Cycle Analysis[1] Cell Line: HeLa cells Concentration: 2.5 μM, 5 μM Incubation Time: 18 hours Result: Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Cell Cytotoxicity Assay[1] Cell Line: HeLa and HT-29 cells Concentration: 500 nM, 625 nM Incubation Time: 96 hours Result: Enhanced cytotoxicity of DNA damage. |
| In Vivo | SB-218078 (5 mg/kg; intraperitoneal injection; for 16 hours; C57/Bl6 mice) treatment could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen in Myc-induced lymphomas mouse model[2]. Animal Model: C57/Bl6 mice injected with ARF-/- lymphomas[2] Dosage: 5 mg/kg Administration: Intraperitoneal injection; for 16 hours Result: Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma. |
| References |
| Molecular Formula | C24H15N3O3 |
|---|---|
| Molecular Weight | 393.39400 |
| Exact Mass | 393.11100 |
| PSA | 69.02000 |
| LogP | 4.36310 |
| Index of Refraction | 1.97 |