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5.32089

Dual DYRK/CLK inhibitor, Cpd 23

Synonyma:

Dual DYRK/CLK inhibitor, Cpd 23, Pre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor

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O této položce

Empirický vzorec (Hillův zápis):
C10H8O2S
Číslo CAS:
56363-81-6
Molekulová hmotnost:
192.23
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD24717135
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light
Technický servis
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assay

≥95% (HPLC)

Quality Level

100

form

powder

potency

60 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 50 mg/mL

storage temp.

−20°C

SMILES string

O=C(C)C1=CC2=CC(O)=CC=C2S1

General description

A cell permeable 5-hydroxybenzothiophenylethanone that acts as a dual inhibitor of Cdc2-like kinase 1 (Clk1; IC50 = 60 nM) and dual specificity tyrosine phosphorylation-regulated kinases 1A/1B (Dyrk1A/1B; IC50 = 200 and 100 nM, respectively). Also inhibits Clk4 with high potency. Exhibits much reduced inhibitory effect on Haspin ( IC50 = 800 nM) and has much reduced inhibitory effect on other kinases even at higher concentration (~ 5 µM). Causes a complete disappearance of incomplete and alternatively spliced transcripts and is shown to enhance the generation of the mature Clk1 mRNA splicing product (EC50 = 8.9 µM) in cells.
A cell permeable, dual inhibitor of Cdc2-like kinase 1 (Clk1; IC₅₀ = 60 nM) and dual specificity tyrosine phosphorylation-regulated kinases 1A/1B (Dyrk1A/1B; IC₅₀ = 200 and 100 nM, respectively).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
DYRK/CLK

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Schmitt, C., et al. 2014. ACS Med. Chem. Lett.5, 963.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Skladovací třída

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Související obsah

Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System

A major focus of breast cancer research is to understand the mechanisms responsible for disease progression and drug resistance. Toward that end, it has been found that approximately two thirds of all human breast carcinomas overexpress the Estrogen Receptor α (ERα) protein and it remains the primary pharmacological target for endocrine therapy1,2. The normal cellular function of ERα is as a transcription factor that mediates a wide variety of physiological processes, many of which are dependent upon phosphorylation of the receptor at specific amino acid residues3,4. Indeed, ERα is known to be phosphorylated at a multitude of different sites, yet how these all correlate to disease remains unclear5. Here, we interrogated multiple sites of ERα for phosphorylation status by screening an extensive panel of different breast cancer patient samples and other non-breast cancer tissue microarray (TMA) slide samples to determine their relevance to disease.

Globální číslo obchodní položky

Skladová položkaGTIN
532089000104055977287158