Cat. No.: HY-107407

SB-218078

5 Cited Publications

Customer Review

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.

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

Purity: 98.30%
CAS No.: 135897-06-2
Formula: C₂₄H₁₅N₃O₃
Molecular Weight:393.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SB-218078 Chemical Structure

CAS No.: 135897-06-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Chk1

15 nM (IC₅₀)

Cdc2

250 nM (IC₅₀)

PKC

1000 nM (IC₅₀)

Apoptosis

All Checkpoint Kinase (Chk) Isoforms :

All CDK Isoforms :

All PKC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.7 μM Compound: 5	In vitro antiproliferative activity against HCT116 ( human colon) cell line. In vitro antiproliferative activity against HCT116 ( human colon) cell line.	[PMID: 14552792]
NCI-H460	IC₅₀	1.64 μM Compound: 5	In vitro antiproliferative activity against NCI-460 (human lung) cell line. In vitro antiproliferative activity against NCI-460 (human lung) cell line.	[PMID: 14552792]

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.

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.

Chemical Information

CAS No. 135897-06-2
Appearance Solid
Molecular Weight 393.39
Formula C₂₄H₁₅N₃O₃
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

Publications (5)

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Cell Rep

Acetylation at lysine 27 on maternal H3.3 regulates minor zygotic genome activation. [Abstract]

2025 Jan 28;44(1):115148. PMID: 39932187
J Cell Biol

DNA damage promotes microtubule dynamics through a DNA-PK-AKT axis for enhanced repair. [Abstract]

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
Patent

US20240174977A1.
bioRxiv

2023 Nov 9.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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SB-218078

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) SB-218078

All Checkpoint Kinase (Chk) Isoforms

All CDK Isoforms

All PKC Isoforms