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UPGL00004

Catalog No. T17206 CAS 1890169-95-5

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.

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UPGL00004, CAS 1890169-95-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 455.00
100 mg	In stock	$ 672.00
1 mL * 10 mM (in DMSO)	In stock	$ 85.00

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Purity: 97.44%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.
Targets&IC50	Glutaminase C:（kd）27 nM, Glutaminase C:29 nM, Glutaminase C:29 nM, Glutaminase C:27 nM（kd）
In vitro	UPGL00004 inhibits MDA-MB-231, HS578T, and TSE cells (IC50s: 70, 129, and 262 nM, respectively).[1]
In vivo	In a triple-negative breast cancer patient-derived tumor graft model, the combination of UPGL00004 (1 mg/kg body weight) and Bevacizumab (2.5 mg/kg body weight) via intraperitoneal injection completely prevent any detectable increase in tumor size.[1]

Molecular Weight	534.66
Formula	C25H26N8O2S2
CAS No.	1890169-95-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 112.5 mg/mL (210.4 mM), Sonication is recommended.

References and Literature

1. Huang Q, et al. Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism. J Biol Chem. 2018 Mar 9;293(10):3535-3545. 2. McDermott LA,et al. Design and evaluation of novel glutaminase inhibitors. Bioorg Med Chem. 2016;24(8):1819-1839.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Cancer Metabolism Compound Library

Related Products

Related compounds with same targets

Telaglenastat BPTES 6-Diazo-5-oxo-L-nor-Leucine Glutaminase-IN-3 L-Albizziin BJJF078 ZED-1227 GLS1 Inhibitor-7

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

UPGL00004 1890169-95-5 Others Proteases/Proteasome Glutaminase UPGL 00004 UPGL-00004 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.