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Glutaminase C inhibitor 968

Chemical Structure : Glutaminase C inhibitor 968

CAS No.: 311795-38-7

Glutaminase C inhibitor 968 (Compound 968)

Catalog No.: PC-43146Not For Human Use, Lab Use Only.

Glutaminase C inhibitor 968 is a small molecule allosteric inhibitor of glutaminase C (GAC) catalytic activity with Kd of 3 uM, specifically inhibited the growth of transformed cells and various cancer cells by blocking GAC activation.

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Biological Activity

Glutaminase C inhibitor 968 is a small molecule allosteric inhibitor of glutaminase C (GAC) catalytic activity with Kd of 3 uM, specifically inhibited the growth of transformed cells and various cancer cells by blocking GAC activation.
Glutaminase C inhibitor 968 inhibits Rho GTPase-dependent transformation and glutaminolysis, blocks the cellular transformation induced by the Rho family-GEF oncogenic Dbl at 1-10 uM.
Glutaminase C inhibitor 968 preferentially binds to the monomeric state of GAC.
Glutaminase C inhibitor 968 reduces the size of the tumors in mouse xenograft lymphoma.

Physicochemical Properties

M.Wt 475.4201
Formula C27H27BrN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzo[a]phenanthridin-4(1H)-one, 5-[3-bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethyl-

References

1. Wang JB, et al. Cancer Cell. 2010 Sep 14;18(3):207-19.

2. Stalnecker CA, et al. Proc Natl Acad Sci U S A. 2015 Jan 13;112(2):394-9.

3. Han T, et al. Oncotarget. 2017 Apr 25;8(17):28063-28073.

4. Effenberger M, et al. Oncotarget. 2017 Aug 24;8(49):85858-85867.

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