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MedKoo Cat#: 562397 | Name: GLS-IN-968
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GLS-IN-968 is an allosteric inhibitor of glutaminase (GLS). It acts by blocking Rho-GTPase-dependent transformation of fibroblasts and suppressing breast cancer cell growth and invasive activity in vitro.

Chemical Structure

GLS-IN-968
GLS-IN-968
CAS#311795-38-7

Theoretical Analysis

MedKoo Cat#: 562397

Name: GLS-IN-968

CAS#: 311795-38-7

Chemical Formula: C27H27BrN2O

Exact Mass: 474.1307

Molecular Weight: 475.43

Elemental Analysis: C, 68.21; H, 5.72; Br, 16.81; N, 5.89; O, 3.37

Price and Availability

Size Price Availability Quantity
5mg USD 285.00 2 Weeks
10mg USD 500.00 2 Weeks
25mg USD 950.00 2 Weeks
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Related CAS #
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Synonym
GLS-IN-968; GLS IN 968; GLSIN968; Glutaminase inhibitor-968; Glutaminase inhibitor 968; GLS inhibitor 968; Glutaminase inhibitor compound 968; Glutaminase C-IN-1
IUPAC/Chemical Name
5-[3-Bromo-4-(dimethylamino)phenyl]-2,3,5,6-tetrahydro-2,2-dimethylbenzo[a]phenanthridin-4(1H)-one
InChi Key
NVFRRJQWRZFDLM-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H27BrN2O/c1-27(2)14-19-24-18-8-6-5-7-16(18)9-11-21(24)29-26(25(19)23(31)15-27)17-10-12-22(30(3)4)20(28)13-17/h5-13,26,29H,14-15H2,1-4H3
SMILES Code
O=C1C(C(C2=CC=C(N(C)C)C(Br)=C2)NC3=C4C5=CC=CC=C5C=C3)=C4CC(C)(C)C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
In vitro activity:
Treatment of primary MM cells with 968 (glutaminase C-IN-1) also induced apoptosis (Figure 1e). In 13 primary patient samples, there was on average a 62% decrease in viable cells in the presence of 10 μM 968 (p= 0.01 to DMSO treatment on non-normalized data). Treatment of five PBMC samples with 968 decreased the percentage of viable cells only to 94% compared to the DMSO control. Reference: Oncotarget. 2017 Aug 24;8(49):85858-85867. https://pubmed.ncbi.nlm.nih.gov/29156762/
In vivo activity:
In xenograft mouse models of endometrial cancer, compound 968 significantly suppressed tumor growth. Reference: Anticancer Agents Med Chem. 2022 May 13. https://pubmed.ncbi.nlm.nih.gov/35570522/
Solvent mg/mL mM
Solubility
DMF 16.0 33.65
DMF:PBS (pH 7.2) (1:2) 0.3 0.63
DMSO 24.9 52.33
Ethanol 0.5 1.05
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 475.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Effenberger M, Bommert KS, Kunz V, Kruk J, Leich E, Rudelius M, Bargou R, Bommert K. Glutaminase inhibition in multiple myeloma induces apoptosis via MYC degradation. Oncotarget. 2017 Aug 24;8(49):85858-85867. doi: 10.18632/oncotarget.20691. PMID: 29156762; PMCID: PMC5689652. 2. Han T, Guo M, Zhang T, Gan M, Xie C, Wang JB. A novel glutaminase inhibitor-968 inhibits the migration and proliferation of non-small cell lung cancer cells by targeting EGFR/ERK signaling pathway. Oncotarget. 2017 Apr 25;8(17):28063-28073. doi: 10.18632/oncotarget.14188. PMID: 28039459; PMCID: PMC5438631. 3. Guo H, Li W, Pan G, Wang C, Li D, Liu N, Sheng X, Yuan L. The Glutaminase Inhibitor Compound 968 Exhibits Potent in vitro and in vivo Anti-tumor Effects in Endometrial Cancer. Anticancer Agents Med Chem. 2022 May 13. doi: 10.2174/1871520622666220513163341. Epub ahead of print. PMID: 35570522.
In vitro protocol:
1. Effenberger M, Bommert KS, Kunz V, Kruk J, Leich E, Rudelius M, Bargou R, Bommert K. Glutaminase inhibition in multiple myeloma induces apoptosis via MYC degradation. Oncotarget. 2017 Aug 24;8(49):85858-85867. doi: 10.18632/oncotarget.20691. PMID: 29156762; PMCID: PMC5689652. 2. Han T, Guo M, Zhang T, Gan M, Xie C, Wang JB. A novel glutaminase inhibitor-968 inhibits the migration and proliferation of non-small cell lung cancer cells by targeting EGFR/ERK signaling pathway. Oncotarget. 2017 Apr 25;8(17):28063-28073. doi: 10.18632/oncotarget.14188. PMID: 28039459; PMCID: PMC5438631.
In vivo protocol:
1. Guo H, Li W, Pan G, Wang C, Li D, Liu N, Sheng X, Yuan L. The Glutaminase Inhibitor Compound 968 Exhibits Potent in vitro and in vivo Anti-tumor Effects in Endometrial Cancer. Anticancer Agents Med Chem. 2022 May 13. doi: 10.2174/1871520622666220513163341. Epub ahead of print. PMID: 35570522.
1: Han T, Guo M, Zhang T, Gan M, Xie C, Wang JB. A novel glutaminase inhibitor-968 inhibits the migration and proliferation of non-small cell lung cancer cells by targeting EGFR/ERK signaling pathway. Oncotarget. 2017 Apr 25;8(17):28063-28073. doi: 10.18632/oncotarget.14188. PubMed PMID: 28039459; PubMed Central PMCID: PMC5438631. 2: Xie C, Jin J, Bao X, Zhan WH, Han TY, Gan M, Zhang C, Wang J. Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer. Oncotarget. 2016 Jan 5;7(1):610-21. doi: 10.18632/oncotarget.6311. PubMed PMID: 26575584; PubMed Central PMCID: PMC4808021.