553509

Ras/Rac Transformation Blocker, SCH 51344

A cell-permeable pyrazoloquinoline compound that acts as an effective blocker of Ras-induced malignant transformation and inhibits Ras/Rac-dependent dissociation of EMS1 from the actin-myosin II complex and membrane ruffling.

• Synonym(s): Ras/Rac Transformation Blocker, SCH 51344, 6-Methoxy-4-(2-((2-hydroxyethoxyl)-ethyl)amino)-3-methyl-1H-pyrazolo[3,4-b]quinoline
• Empirical Formula (Hill Notation): C₁₆H₂₀N₄O₃
• CAS Number: 171927-40-5
• Molecular Weight: 316.36
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: DMSO: 20 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C16H20N4O3/c1-10-14-15(17-5-7-23-8-6-21)12-9-11(22-2)3-4-13(12)18-16(14)20-19-10/h3-4,9,21H,5-8H2,1-2H3,(H2,17,18,19,20)
• InChI key: YWEGXZZAORIRQR-UHFFFAOYSA-N

Description

General description

A cell-permeable pyrazoloquinoline compound that acts as an effective blocker of Ras-induced malignant transformation and inhibits Ras/Rac-dependent dissociation of EMS1 from the actin-myosin II complex and membrane ruffling. The effect of SCH 51344 is limited to Ras/Rac pathway(s) other than those involving ERK and JNK. Shown to directly target human mutT homolog MTH1/NUDT1 with a K_d of 49 nM and inhibit its catalytic activity (IC₅₀ for pyrophosphate release during nucleotide triphosphate hydrolysis = 215, 410 and 675 nM against dGTP, 8-oxo-dGTP and 2-OH-dATP substrates, respectively).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Ras/Rac

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Huber, K. V. M., et al. 2014. Nature In press.
He, H., et al. 1998. Mol. Cell. Biol.18, 3829.
Walsh, A.B., et al. 1997. Oncogene15, 2553.
Chandra Kumar, C., et al. 1995. Cancer Res.55, 5106.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable