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

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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SB-218078 Chemical Structure

SB-218078 Chemical Structure

CAS No. : 135897-06-2

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Based on 3 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-218078 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (101.68 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5420 mL 12.7100 mL 25.4201 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

COA (264 KB) Elemental Analysis Report (122 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5420 mL 12.7100 mL 25.4201 mL 63.5502 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL 12.7100 mL
10 mM 0.2542 mL 1.2710 mL 2.5420 mL 6.3550 mL
15 mM 0.1695 mL 0.8473 mL 1.6947 mL 4.2367 mL
20 mM 0.1271 mL 0.6355 mL 1.2710 mL 3.1775 mL
25 mM 0.1017 mL 0.5084 mL 1.0168 mL 2.5420 mL
30 mM 0.0847 mL 0.4237 mL 0.8473 mL 2.1183 mL
40 mM 0.0636 mL 0.3178 mL 0.6355 mL 1.5888 mL
50 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2710 mL
60 mM 0.0424 mL 0.2118 mL 0.4237 mL 1.0592 mL
80 mM 0.0318 mL 0.1589 mL 0.3178 mL 0.7944 mL
100 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6355 mL
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SB-218078 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-218078135897-06-2SB218078SB 218078Checkpoint Kinase (Chk)CDKPKCApoptosisCyclin dependent kinaseProtein kinase CChk1phosphorylationcdc25CCdc2G2cyclearrestDNA-damagingapoptosisInhibitorinhibitorinhibit

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