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Sigma-Aldrich

Brk Inhibitor, Cpd 4f

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Synonym(s):
Brk Inhibitor, Cpd 4f, PTK6 Inhibitor, Breast Tumor Kinase Inhibitor
Empirical Formula (Hill Notation):
C17H13N3O
Molecular Weight:
275.30

assay

≥97% (HPLC)

Quality Level

form

powder

potency

3.15 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light beige

solubility

DMSO: 100 mg/mL

storage temp.

−20°C

General description

A cell permeable pyridoindole based compound that acts as a highly potent and selective inhibitor of breast tumor kinase (Brk; IC50 = 3.15 nM) with minimal or no effect against a panel of more than 30 other protein kinases (IC50 = <10 µM for PIM2, NEK1 and2, CAMK4, MAPKAPK3 and 5 and MARK1, 3, and 5). Does not affect the activity of Akt isoforms, AGC kinases, ERK1 and 2, JNK 1 and 2 and HIPK isoforms. Displays anti-proliferative activity against multiple breast cancer cell lines (GI50 = 990 nM; 1.02 µM, and 1.58 µM for MCF7, HS-578/T, BT-549, respectively).
A cell permeable pyridoindole based compound that acts as a highly potent and selective inhibitor of breast tumor kinase (Brk; IC50 = 3.15 nM) with minimal or no effect against a panel of more than 30 other protein kinases (IC50 = <10 µM for PIM2, NEK1 and2, CAMK4, MAPKAPK3 and 5 and MARK1, 3, and 5). Does not affect the activity of Akt isoforms, AGC kinases, ERK1 and 2, JNK 1 and 2 and HIPK isoforms. Displays anti-proliferative activity against multiple breast cancer cell lines (GI50 = 990 nM; 1.02 µM, and 1.58 µM for MCF7, HS-578/T, BT-549, respectively).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Brk

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are good for up to 2 weeks at -70°C.
Use only fresh DMSO for reconstitution.

Other Notes

Mahmoud, K. A., et al. 2014. Bioorg. Med. Chem. Lett.24, 1948.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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