Domatinostat

SKU: orb1300834

Description

Domatinostat (4SC202) is a selective class I HDAC inhibitor targeting HDAC1, HDAC2, and HDAC3, and also inhibits LSD1. It has been investigated in Phase 1 clinical trials for oncology research, with studies demonstrating its activity in both in vitro cellular assays and in vivo cancer models.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 910462-43-0
• MW: 447.51
• Purity: 99.74% (May vary between batches)
• Formula: C₂₃H₂₁N₅O₃S
• SMILES: Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1
• Target: Apoptosis,HDAC
• Solubility: DMSO:82 mg/mL (183.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.37 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC2:1.12 μM|HDAC1:1.20 μM|HDAC9:50 μM|HDAC5:11.3 μM|HDAC10:21 μM|HDAC3:0.57 μM|HDAC11:9.7 μM
• In Vivo:
  In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model.
• In Vitro:
  In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM.

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

Domatinostat, 4SC202, 4SC-202, 4SC-202 (free base), 4SC 202, Apoptosis, inhibit, Histone deacetylases, Inhibitor, HDAC, HDAC3, HDAC5, HDAC2, HDAC1, HDAC11

Compound Identifiers

PubChem CID

15985904