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Glutaminase C-IN-1

Product Name
Glutaminase C-IN-1
CAS No.
311795-38-7
Chemical Name
Glutaminase C-IN-1
Synonyms
CS-2083;GLS-IN-968;Compound 968;GAC Inhibitor 968;Glutaminase C-IN-1;Glutaminase C-IN-1 (968);Glutaminase C inhibitor 1;glutaminase inhibitor 968;Glutaminase Inhibitor Compound 968;Glutaminase Inhibitor 968 >=98% (HPLC)
CBNumber
CB32561506
Molecular Formula
C27H27BrN2O
Formula Weight
475.42
MOL File
311795-38-7.mol
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Glutaminase C-IN-1 Property

Boiling point:
623.2±55.0 °C(Predicted)
Density 
1.39±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
Soluble in DMSO (up to 11 mg/ml) or in Ethanol (up to 1 mg/ml with warming)
form 
powder
pka
4.09±0.42(Predicted)
color 
white to beige
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1327
Product name
Glutaminase Inhibitor 968
Purity
≥98% (HPLC)
Packaging
5MG
Price
$115
Updated
2023/06/20
Sigma-Aldrich
Product number
SML1327
Product name
Glutaminase Inhibitor 968
Purity
≥98% (HPLC)
Packaging
25MG
Price
$451
Updated
2023/06/20
Cayman Chemical
Product number
17199
Product name
Glutaminase Inhibitor Compound 968
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
17199
Product name
Glutaminase Inhibitor Compound 968
Purity
≥98%
Packaging
5mg
Price
$70
Updated
2024/03/01
Cayman Chemical
Product number
17199
Product name
Glutaminase Inhibitor Compound 968
Purity
≥98%
Packaging
10mg
Price
$122
Updated
2024/03/01
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Glutaminase C-IN-1 Chemical Properties,Usage,Production

Description

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

Uses

Glutaminase inhibitor 968 has been used to study the role of glutamine metabolism in macrophage activation.

Definition

ChEBI: 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one is a partially hydrogenated benzophenanthridine carrying an oxo group at C-4, geminal methyl groups at C-2 and a 3-bromo-4-(dimethylamino)phenyl group at C-5. It has a role as an EC 3.5.1.2 (glutaminase) inhibitor.

General Description

Glutaminase Inhibitor 968 belongs to the benzophenanthridinone family.

Biochem/physiol Actions

Glutaminase Inhibitor 968 is an allosteric inihibitor of the mitochondrial enzyme glutaminase C (GAC), which is overexpressed in a number of cancer cell lines. Glutaminase Inhibitor 968 shows 21% inhibition at 10 μM, 94% at 25 μM. Glutaminase Inhibitor 968 blocked human cancer cell proliferation in culture, and in inhibited tumor formation in mouse xenograft models.

storage

Store at -20°C

References

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 Wang et al. (2010), Targeting mitochondrial glutaminase activity inhibits oncogenic transformation; Cancer Cell, 18 207 Katt et al. (2012), Dibenzophenanthridines as inhibitors of glutaminase C and cancer cell proliferation; Cancer Ther., 11 1269 Lukey et al. (2019), Liver-Type Glutaminase GLS2 Is a Druggable Metabolic Node in Luminal-Subtype Breast Cancer; Cell Reports, 29 76 Xie et al. (2016), Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer; Oncotarget, 7 610

Glutaminase C-IN-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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Glutaminase C-IN-1 Suppliers

Beijing HwrkChemical Technology Co., Ltd
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View Lastest Price from Glutaminase C-IN-1 manufacturers

Career Henan Chemical Co
Product
Glutaminase C-IN-1 311795-38-7
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
Customized
Release date
2019-09-04

311795-38-7, Glutaminase C-IN-1Related Search:


  • 5-[3-BroMo-4-(diMethylaMino)phenyl]-2,3,5,6-tetrahydro-2,2-diMethylbenzo[a]phenanthridin-4(1H)-one
  • Glutaminase C-IN-1
  • Glutaminase C-IN-1 (968)
  • Glutaminase Inhibitor Compound 968
  • glutaminase inhibitor 968
  • CS-2083
  • 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-1,3,5,6-tetrahydrobenzo[a]phenanthridin-4-one
  • Glutaminase C inhibitor 1
  • Compound 968
  • Benzo[a]phenanthridin-4(1H)-one, 5-[3-bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethyl-
  • Glutaminase Inhibitor 968 >=98% (HPLC)
  • GLS-IN-968
  • GAC Inhibitor 968
  • Compound968,Glutaminase,Glutaminase CIN1,Glutaminase C IN 1,Compound-968,inhibit,Inhibitor
  • 311795-38-7