1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. UPGL00004

UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.

For research use only. We do not sell to patients.

UPGL00004 Chemical Structure

UPGL00004 Chemical Structure

CAS No. : 1890169-95-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 160 In-stock
25 mg USD 320 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines[1].

IC50 & Target

IC50: 29 nM (Glutaminase C)[1]
Kd: 27 nM (Glutaminase C)[1]

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
70 nM
Compound: 7c
Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
[PMID: 26988803]
In Vitro

UPGL00004 inhibits MDA-MB-231, HS578T and TSE cells with IC50s of 70, 129, and 262 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 in a triple-negative breast cancer patient-derived tumor graft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

534.66

Formula

C25H26N8O2S2

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(NC1=NN=C(N2CCC(NC3=NN=C(NC(CC4=CC=CC=C4)=O)S3)CC2)S1)CC5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (233.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8703 mL 9.3517 mL 18.7035 mL
5 mM 0.3741 mL 1.8703 mL 3.7407 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8703 mL 9.3517 mL 18.7035 mL 46.7587 mL
5 mM 0.3741 mL 1.8703 mL 3.7407 mL 9.3517 mL
10 mM 0.1870 mL 0.9352 mL 1.8703 mL 4.6759 mL
15 mM 0.1247 mL 0.6234 mL 1.2469 mL 3.1172 mL
20 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3379 mL
25 mM 0.0748 mL 0.3741 mL 0.7481 mL 1.8703 mL
30 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5586 mL
40 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
50 mM 0.0374 mL 0.1870 mL 0.3741 mL 0.9352 mL
60 mM 0.0312 mL 0.1559 mL 0.3117 mL 0.7793 mL
80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5845 mL
100 mM 0.0187 mL 0.0935 mL 0.1870 mL 0.4676 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
UPGL00004
Cat. No.:
HY-119377
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