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Chemical Structure| 72926-24-0 Chemical Structure| 72926-24-0

Structure of K858 (Racemic)
CAS No.: 72926-24-0

Chemical Structure| 72926-24-0

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K858 is a selective and ATP-uncompetitive mitotic kinesin Eg5 inhibitor with IC50 value of 1.3 μM.

Synonyms: K858

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Product Details of K858 (Racemic)

CAS No. :72926-24-0
Formula : C13H15N3O2S
M.W : 277.34
SMILES Code : CC(NC1=NN(C(C)=O)C(C2=CC=CC=C2)(C)S1)=O
Synonyms :
K858
MDL No. :MFCD00181155
InChI Key :JEFVYQYZCAVNTP-UHFFFAOYSA-N
Pubchem ID :2930014

Safety of K858 (Racemic)

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of K858 (Racemic)

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
AGS human gastric adenocarcinoma cells 1, 3, 5, 8 μM 24 hours Immunofluorescence analysis of β-tubulin revealed that K858 treatment resulted in monopolar spindle formation, indicating mitotic arrest. Molecules. 2019 Oct 31;24(21):3948
AGS human gastric adenocarcinoma cells 0.5, 5, 50, 100 μM 24, 48, 72 hours Evaluate cell viability, found that compounds 2 and 41 significantly reduced AGS cell viability, with IC50 values of 3 μM and 6 μM, respectively. Molecules. 2019 Oct 31;24(21):3948
vascular smooth muscle cells (VSMCs) 1 μM 24 hours Inhibition of KIF11 activity partially reversed the pro-cycle progression and pro-proliferation effects of PDGF-BB on VSMCs Front Pharmacol. 2024 Aug 6;15:1392352
AGS human gastric adenocarcinoma cells 1 and 5 µM 48 and 72 hours Evaluation of antiproliferative effect, showing significant reduction in metabolic activity Molecules. 2022 Jan 31;27(3):957

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57 mice Mouse carotid artery injury model Intraperitoneal injection 50 mg/kg Every other day for 2 weeks Inhibition of KIF11 activity attenuates neointimal formation after vascular injury Front Pharmacol. 2024 Aug 6;15:1392352

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.61mL

0.72mL

0.36mL

18.03mL

3.61mL

1.80mL

36.06mL

7.21mL

3.61mL

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