1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Epigenetics
    Apoptosis
  2. Checkpoint Kinase (Chk)
    CDK
    PKC
    Apoptosis
  3. SB-218078

SB-218078 

Cat. No.: HY-107407 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

SB-218078 Chemical Structure

SB-218078 Chemical Structure

CAS No. : 135897-06-2

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10 mM * 1  mL in DMSO USD 467 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target[1]

Chk1

15 nM (IC50)

Cdc2

250 nM (IC50)

PKC

1000 nM (IC50)

Apoptosis

 

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.
Molecular Weight

393.39

Formula

C₂₄H₁₅N₃O₃

CAS No.

135897-06-2

SMILES

O=C1NC(C(C2=C3N(C4CCC5O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References

Purity: >98.0%

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Keywords:

SB-218078SB218078SB 218078Checkpoint Kinase (Chk)CDKPKCApoptosisCyclin dependent kinaseProtein kinase CChk1phosphorylationcdc25CCdc2G2cyclearrestDNA-damagingapoptosisInhibitorinhibitorinhibit

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SB-218078
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HY-107407
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