BTO-1

Names

[ Name ]:
BTO-1

[Synonym ]:
BTO-1
5-cyano-7-nitro-3-oxy-benzothiazole-2-carboxylic acid amide
HMS3260F21
HMS3229L17
5-Cyano-7-nitro-2-benzothiazolecarboxamide-3-oxide

Biological Activity

[Description]:

BTO-1 is a Polo-like kinase (Plk) inhibitor. BTO-1 is primarily used for phosphorylation and dephosphorylation applications[1][2].

[Related Catalog]:

Research Areas >> Others

Signaling Pathways >> Cell Cycle/DNA Damage >> Polo-like Kinase (PLK)

[Target]

Plx1

[In Vitro]

BTO-1 (50 μM; 4 hours; U20S cells) results in monopolar spindles in a comparable fraction of mitotic cells. BTO-1(20 μM; 1 hour; PTK cells) shows a dose-dependent reduction in phospho-Cdc25C. BTO-1(25 μM; 1 hour; PTK cells) shows about 20 % reduction in H3 phosphorylation compared to control cells. BTO-1 in HeLa cells results in a blockage of Rho and Rho-GEF recruitment, which is essential for the assembly of a functional contractile ring[1][2].

[References]

[1]. Peters, U., et al. Probing cell-division phenotype space and Polo-like kinase function using small molecules. Nat Chem Biol 2, 618–626 (2006).

[2]. Brennan IM, et al. Polo-like kinase controls vertebrate spindle elongation and cytokinesis. PLoS One. 2007;2(5):e409. Published 2007 May 2.

Chemical & Physical Properties

[ Molecular Formula ]:
C₉H₄N₄O₄S

[ Molecular Weight ]:
264.21700

[ Exact Mass ]:
263.99500

[ PSA ]:
166.40000

[ LogP ]:
2.43208

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H312-H315-H319-H332-H335

[ Precautionary Statements ]:
P261-P280-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
20/21/22-36/37/38

[ Safety Phrases ]:
26-36/37

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Plk1 and CK2 act in concert to regulate Rad51 during DNA double strand break repair.

Mol. Cell. 45 , 371-383, (2012)

Homologous recombination (HR) plays an important role in the maintenance of genome integrity. HR repairs broken DNA during S and G2 phases of the cell cycle but its regulatory mechanisms remain elusiv...

Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.

Nat. Chem. Biol. 2 , 608-617, (2006)

Polo-like kinases (Plks) have several functions in mitotic progression and are upregulated in many tumor types. Small-molecule Plk inhibitors would be valuable as tools for studying Plk biology and fo...

Two High Throughput Screen Assays for Measurement of TNF-α in THP-1 Cells.

Curr. Chem. Genomics 5 , 21-9, (2011)

Tumor Necrosis Factor-α (TNF-α), a secreted cytokine, plays an important role in inflammatory diseases and immune disorders, and is a potential target for drug development. The traditional assays for ...