BRK INHIBITOR CPD 4F (C15-1305-038)

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

Molecular Weight: 275.30. Empirical Formula: C₁₇H₁₃N₃O. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.