OTUB1/USP8-IN-1

SKU: orb1744671

Description

OTUB1/USP8-IN-1 is a highly potent dual inhibitor of the deubiquitinases OTUB1 and USP8, exhibiting sub-nanomolar IC50 values. This compound serves as a valuable research tool for investigating deubiquitinase function in oncology, particularly in non-small cell lung cancer (NSCLC) studies, with applications in both cellular and biochemical assays.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2858800-98-1
• MW: 426.83
• Purity: 98.82% (May vary between batches)
• Formula: C₂₂H₁₆ClFN₂O₄
• SMILES: O=C1C2=C(OC(=N2)C3=C(Cl)C(O[C@H]4CN(C)CC4)=CC=C3F)C(=O)C=5C1=CC=CC5
• Target: DUB
• Solubility: DMSO:30 mg/mL (70.29 mM)

Bioactivity

• Target IC50:
  H23 cells:431 nM|A549 cells:1004 nM|EBC-1 cells:172 nM|H1703 cells:145 nM|H1975 cells (EGFR):118 nM
• In Vivo:
  OTUB1/USP8-IN-1 (5 mg/kg; intraperitoneal injection; QD and BID, for 2 weeks) reduced the total tumor weight and average tumor volume in BALB/c nude mice by over twofold with BID dosing.
• In Vitro:
  OTUB1/USP8-IN-1 (10 nM-10 μM; 72 hours) inhibited the proliferation of H1975, H1703, EBC-1, H23, and A549 cells with IC50 values of 118, 145, 172, 431, and 1004 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

USP8

Compound Identifiers

PubChem CID

165437860