Domatinostat tosylate

SKU: orb1302825

Description

Domatinostat tosylate

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1186222-89-8
• MW: 619.71
• Purity: 97.35%
• Formula: C₃₀H₂₉N₅O₆S₂
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.Cn1cc(cn1)-c1ccc(cc1)S(=O)(=O)n1ccc(\C=C\C(=O)Nc2ccccc2N)c1
• Target: HDAC,Apoptosis
• Solubility: H2O:Insoluble;DMSO:50 mg/mL (80.68 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.23 mM)

Bioactivity

• Target IC50:
  HDAC9:50 μM|HDAC5:11.3 μM|HDAC1:1.2 μM|HDAC2:1.12 μM|HDAC11:9.7 μM|HDAC10:21 μM|HDAC3:0.57 μM
• In Vivo:
  4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened.
• In Vitro:
  Domatinostat provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat. Domatinostat-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat in HT-29 cells. Notably, Domatinostat, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity. Domatinostat obviously reduces the proliferation of all epithelial and mesenchymal UC cell lines (IC50: 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity. Domatinostat treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D.

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

Apoptosis, 4SC 202, 4SC 202 Tosylate, 4SC202, 4SC-202, 4SC202 Tosylate, Domatinostat, HDAC9, HDAC, HDAC1, HDAC10, HDAC2, HDAC11, HDAC3, HDAC5

Compound Identifiers

PubChem CID

44217246