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Glutaminase C-IN-1, also known as GAC Inhibitor 968, is an allosteric inhibitor of glutaminase C (GAC) belonging to the benzophenanthridinone family. It plays a crucial role in blocking oncogenic transformation induced by Rho GTPases in fibroblasts and B lymphoma cells without affecting normal cells. Its ability to inhibit liver-type glutaminase GLS2 and suppress breast tumor growth in vivo, as well as reverse acquired erlotinib resistance in non-small cell lung cancer, makes it a promising compound in the field of cancer research and treatment.

311795-38-7

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311795-38-7 Usage

Uses

Used in Cancer Research:
Glutaminase C-IN-1 is used as a research tool for studying the role of glutamine metabolism in macrophage activation and its impact on cancer cell growth and proliferation. It helps researchers understand the underlying mechanisms of cancer development and progression.
Used in Anticancer Applications:
Glutaminase C-IN-1 is used as an anticancer agent for its ability to inhibit liver-type glutaminase GLS2, which is involved in breast tumor growth in vivo. By targeting this enzyme, it can potentially suppress tumor growth and improve treatment outcomes for breast cancer patients.
Used in Overcoming Drug Resistance:
Glutaminase C-IN-1 is used as a therapeutic agent to reverse acquired erlotinib resistance in non-small cell lung cancer. This application can help improve the efficacy of existing treatments and provide new options for patients with drug-resistant cancers.
Used in Pharmaceutical Development:
Glutaminase C-IN-1 is used as a lead compound in the development of new drugs targeting glutaminase C, which can potentially be applied in various cancer treatments. Its unique properties and mechanisms of action make it a valuable asset in the search for novel cancer therapies.

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.

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

Check Digit Verification of cas no

The CAS Registry Mumber 311795-38-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,1,1,7,9 and 5 respectively; the second part has 2 digits, 3 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 311795-38:
(8*3)+(7*1)+(6*1)+(5*7)+(4*9)+(3*5)+(2*3)+(1*8)=137
137 % 10 = 7
So 311795-38-7 is a valid CAS Registry Number.

311795-38-7 Well-known Company Product Price

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  • Sigma

  • (SML1327)  Glutaminase Inhibitor 968  ≥98% (HPLC)

  • 311795-38-7

  • SML1327-5MG

  • 983.97CNY

  • Detail
  • Sigma

  • (SML1327)  Glutaminase Inhibitor 968  ≥98% (HPLC)

  • 311795-38-7

  • SML1327-25MG

  • 3,970.98CNY

  • Detail

311795-38-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

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

1.2 Other means of identification

Product number -
Other names QC-219

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:311795-38-7 SDS

311795-38-7Downstream Products

311795-38-7Relevant academic research and scientific papers

INHIBITORS OF KIDNEY-TYPE GLUTAMINASE, GLS-1

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Paragraph 0125, (2016/06/28)

The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

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