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553509

Sigma-Aldrich

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.

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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

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

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 Kd 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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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