GAC Inhibitor 968 | Glutaminase C inhibitor

GAC Inhibitor 968 (311795-38-7) is an allosteric inhibitor of glutaminase C (GAC).1 Inhibition of GAC blocks oncogenic transformation induced by Rho GTPases in fibroblasts and B lymphoma cells with no effect on normal cells.2 Inhibits liver-type glutaminase GLS2 and suppresses breast tumor growth in vivo.3,4 Reverses acquired erlotinib resistance in non-small cell lung cancer.5

References:

  1. Stainecker et al. (2015), Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells; Proc. Natl. Acad. Sci. USA, 112 394
  2. Wang et al. (2010), Targeting mitochondrial glutaminase activity inhibits oncogenic transformation; Cancer Cell, 18 207
  3. Katt et al. (2012), Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation; Cancer Ther., 11 1269
  4. Lukey et al. (2019), Liver-Type Glutaminase GLS2 Is a Druggable Metabolic Node in Luminal-Subtype Breast Cancer; Cell Reports, 29 76
  5. Xie et al. (2016), Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer; Oncotarget, 7 610
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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CAS:
311795-38-7
Catalog Number:
10-1538
Activity:
Glutaminase C inhibitor
Chemical Names:

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

Molecular Weight:
475.42
Molecular Formula:
C27H27BrN2O
Solubility:
Soluble in DMSO (up to 11 mg/ml) or in Ethanol (up to 1 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
98%  TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 year2 as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

GAC Inhibitor 968 | Glutaminase C inhibitor

$60.00$240.00

CAS:
311795-38-7
Catalog Number:
10-1538
Activity:
Glutaminase C inhibitor
Chemical Names:

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

Molecular Weight:
475.42
Molecular Formula:
C27H27BrN2O
Solubility:
Soluble in DMSO (up to 11 mg/ml) or in Ethanol (up to 1 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
98%  TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 year2 as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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