SB-218078
Based on 5 publication(s) in Google Scholar
SB-218078 is a potent, selective, ATP-competitive 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.
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- Pureza: 98.30%
- No. CAS: 135897-06-2
- Fòrmula: C24H15N3O3
- Peso molecular:393.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) SB-218078
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Actividad biológica
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Chk1 15 nM (IC50) |
Cdc2 250 nM (IC50) |
PKC 1000 nM (IC50) |
Apoptosis |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.7 μM
Compound: 5
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In vitro antiproliferative activity against HCT116 ( human colon) cell line.
In vitro antiproliferative activity against HCT116 ( human colon) cell line.
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[PMID: 14552792] |
| NCI-H460 | IC50 |
1.64 μM
Compound: 5
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In vitro antiproliferative activity against NCI-460 (human lung) cell line.
In vitro antiproliferative activity against NCI-460 (human lung) cell line.
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[PMID: 14552792] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:2.5 μM, 5 μM
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Incubation Time:18 hours
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Result:Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition.
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Cell Line:HeLa and HT-29 cells
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Concentration:500 nM, 625 nM
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Incubation Time:96 hours
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Result:Enhanced cytotoxicity of DNA damage.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/Bl6 mice injected with ARF-/- lymphomas[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; for 16 hours
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Result:Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
Chemical Information
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No. CAS 135897-06-2
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Appearance Solid
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Peso molecular 393.39
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Fòrmula C24H15N3O3
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Color Light yellow to yellow
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SMILES
O=C1NC(C(C2=C3N(C4CCC5O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Rep
2025 Jan 28;44(1):115148. PMID: 39932187 -
J Cell Biol
2021 Feb 1;220(2):e201911025. PMID: 33404607 -
Exp Neurol
Hydrogen sulfide ameliorates lipopolysaccharide-induced anxiety-like behavior by inhibiting checkpoint kinase 1 activation in the hippocampus of mice. [Abstract]2024 Jan:371:114586. PMID: 37898396 -
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Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jackson JR, et al. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 2000 Feb 1;60(3):566-72. [Content Brief]
[2]. Murga M, et al. Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors. Nat Struct Mol Biol. 2011 Nov 27;18(12):1331-1335. [Content Brief]
[3]. Preet R, et al. Chk1 inhibitor synergizes quinacrine mediated apoptosis in breast cancer cells by compromising the base excision repair cascade. Biochem Pharmacol. 2016 Apr 1;105:23-33. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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