5.31000

Brk Inhibitor, Cpd 4f

• Synonym(s): Brk Inhibitor, Cpd 4f, PTK6 Inhibitor, Breast Tumor Kinase Inhibitor
• Empirical Formula (Hill Notation): C₁₇H₁₃N₃O
• Molecular Weight: 275.30
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable