UPGL00004

SKU: orb1706492

Description

UPGL00004 is a potent and selective glutaminase C (GAC) inhibitor, demonstrating high affinity with a Kd of 27 nM and inhibiting GAC activity with an IC50 of 29 nM. It effectively suppresses the proliferation of aggressive triple-negative breast cancer cells in vitro, making it a valuable tool for studying cancer metabolism and therapeutic targeting.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1890169-95-5
• MW: 534.66
• Purity: 97.93% (May vary between batches)
• Formula: C₂₅H₂₆N₈O₂S₂
• SMILES: O=C(Cc1ccccc1)Nc1nnc(NC2CCN(CC2)c2nnc(NC(=O)Cc3ccccc3)s2)s1
• Target: Glutaminase
• Solubility: DMSO:112.5 mg/mL (210.41 mM)

Bioactivity

• Target IC50:
  Glutaminase C:29 nM|Glutaminase C:（kd）27 nM|Glutaminase C:29 nM|Glutaminase C:27 nM（kd）
• 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.
• In Vitro:
  UPGL00004 inhibits MDA-MB-231, HS578T, and TSE cells (IC50s: 70, 129, and 262 nM, respectively).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Glutaminase C, UPGL 00004, UPGL00004, UPGL-00004

Compound Identifiers

PubChem CID

121256411