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SB-218078

CAS No. 135897-06-2

SB-218078( SB 218078 | SB218078 )

Catalog No. M11474 CAS No. 135897-06-2

A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    SB-218078
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM.
  • Description
    A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM; less potently inhibits Cdc2 and PKC (IC50=250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 uM; enhances the cytotoxicity of DNA-damaging agents.
  • 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.SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .Cell Cycle Analysis 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 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. Animal Model:C57/Bl6 mice injected with ARF-/- lymphomas Dosage:5 mg/kg Administration:Intraperitoneal injection; for 16 hours Result:Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
  • Synonyms
    SB 218078 | SB218078
  • Pathway
    Angiogenesis
  • Target
    Chk
  • Recptor
    Chk
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    135897-06-2
  • Formula Weight
    393.4
  • Molecular Formula
    C24H15N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1NC(C(C2=C3N([C@@]4([H])CC[C@]5([H])O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=O
  • Chemical Name
    5,6,7,8-tetrahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-13,15(14H)-dione

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Jackson JR, et al. Cancer Res. 2000 Feb 1;60(3):566-72. 2. Fishler T, et al. Oncogene. 2010 Jul 15;29(28):4007-17. 3. Akasaka T, et al. Int J Oncol. 2015 Jan;46(1):63-70.
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