Sigma-Aldrich Brk Inhibitor Cpd 4f

Assay

≥97% (HPLC)

Quality Level

100

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: yesPrimary 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany