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SB 218078

Catalog No.GC11022

checkpoint kinase 1 (Chk1) inhibitor

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SB 218078 Chemical Structure

Cas No.: 135897-06-2

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1mg
$135.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Targets:Chk1, cdc2 and PKC

IC50:15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively

SB 218078 is a potent inhibitor of checkpoint kinase 1, with the IC50 values of 15, 250 and 1000 nM for Chk1, cdc2 and PKC, respectively.

In Vitro: An in vitro kinase assay found that SB 218078 could potently inhibit the phosphorylation of Chk1, with the IC50 of 15 nM. In Hela cells, SB 218078 could cause complete abrogation of G2 cell cycle arrest induced by topotecan, with the minimum concentration of 2.5 μM [1]. Besides, 15 nM SB 218078 could effectively inhibit NKG2D ligand upregulation induced by aphidicolin in fibroblasts [2]. Furthermore, treated GM02188 cells with 2.5 μM SB 218078 could inhibit the formation of HU-induced 53bp1 foci and prevent recovery from replication fork stalling induced by APH [3].

In Vivo: In Myc-induced lymphomas mouse model, treatment with SB 218078 with the dose of 5 mg/kg could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen [4].

Clinical trial: No data available recently

References:
[1] Jackson J R, Gilmartin A G, Imburgia C S, et al.  An Indolocarbazole Inhibitor of Human Checkpoint Kinase (Chk1) Abrogates Cell Cycle Arrest Caused by DNA Damage[J]. Cancer Research, 2000, 60(3): 566-572.
[2] Gasser S, Orsulic S, Brown E J, et al.  The DNA damage pathway regulates innate immune system ligands of the NKG2D receptor[J]. Nature, 2005, 436(7054): 1186-1190.
[3] Alderton G K, Galbiati L, Griffith E, et al.  Regulation of mitotic entry by microcephalin and its overlap with ATR signalling[J]. Nature Cell Biology, 2006, 8(7): 725-733.
[4] Murga M, Campaner S, Lopez-Contreras A J, et al.  Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors[J]. Nature structural & molecular biology, 2011, 18(12): 1331-1335.

Chemical Properties

Cas No. 135897-06-2 SDF
Chemical Name 9,10,11,12-tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
Canonical SMILES O=C(NC1=O)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5C7OC(CC7)N4C8=C3C=CC=C8
Formula C24H15N3O3 M.Wt 393.4
Solubility ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5419 mL 12.7097 mL 25.4194 mL
5 mM 0.5084 mL 2.5419 mL 5.0839 mL
10 mM 0.2542 mL 1.271 mL 2.5419 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 15 reference(s) in Google Scholar.)

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