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Chemical Structure| 850467-66-2 Chemical Structure| 850467-66-2

Structure of TAO Kinase inhibitor 1
CAS No.: 850467-66-2

Chemical Structure| 850467-66-2

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TAO Kinase inhibitor 1 is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. It inhibits TAOK phosphorylation and activation of JNK in vitro, and also prolongs duration of mitosis and increases mitotic cell death in the SKBR3 breast cancer cell line.

Synonyms: CP 43; Compound 43 TAO Kinase Inhibitor

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Product Citations

Product Citations

Begg, Bridget E ; Tracey, Matthew A ; Gao, Shengyan ; Ernest, Svetlana ; Najar, Mohd Altaf ; Burslem, George M , et al.

Abstract: Nuclear speckles are membraneless organelles that act as active splicing hubs especially at sites of high transcription. Emerging views of this dynamic subnuclear structure place it as a hub of RNA processing, impacting steps from transcription to export. To manage this complex microcosm of RNA metabolism, nuclear speckles also require kinases and phosphorylation to execute their functions. The nuclear speckle-localized kinase, TAOK2, mediates the splicing and export of viral transcripts at the nuclear speckle, but its role in the processing of cellular transcripts was unknown. We used siRNA knockdown of TAOK2 and assessed RNA transcripts in both whole cell and nucleocytoplasmic fractions to characterize the complete endogenous effects of TAOK2. We found that TAOK2 knockdown impacts over 10% of the transcriptome, through changes in alternative splicing, export and transcript abundance. Cellular and biochemical phosphoproteomics further revealed nuclear speckle scaffolding proteins SRRM1 and SRRM2 as potential direct phosphorylation targets of TAOK2, mediating its large effects on speckle integrity and speckle-localized splicing. Indeed, knockdown of TAOK2 perturbs almost all speckle-resident serine/arginine (SR)-rich proteins while leaving heterogeneous ribonucleoproteins unperturbed. Altogether, we propose that phosphorylation of SRRM1/2 by TAOK2 plays a structural maintenance role that impacts SR protein-driven exon inclusion at the nuclear speckle.

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Product Details of TAO Kinase inhibitor 1

CAS No. :850467-66-2
Formula : C25H24N2O2
M.W : 384.47
SMILES Code : O=C(CNC(C1=CC=C(C2=CC=CC=C2)C=C1)=O)NC(CCC3)C4=C3C=CC=C4
Synonyms :
CP 43; Compound 43 TAO Kinase Inhibitor
MDL No. :MFCD15612807
InChI Key :WQKXOAJVNFOHNZ-UHFFFAOYSA-N
Pubchem ID :46673962

Safety of TAO Kinase inhibitor 1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of TAO Kinase inhibitor 1

MAPK

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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