Pracinostat

SKU: orb1307242

Description

Pracinostat (SB939) is an orally bioavailable HDAC inhibitor with potent anti-tumor activity. It demonstrates efficacy in preclinical models of hematological malignancies and solid tumors, supporting its research use in oncology and epigenetics.

Research Area

Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 929016-96-6
• MW: 358.48
• Purity: 99.67% (May vary between batches)
• Formula: C₂₀H₃₀N₄O₂
• SMILES: CCCCc1nc2cc(\C=C\C(=O)NO)ccc2n1CCN(CC)CC
• Target: HDAC,Antibacterial,Apoptosis
• Solubility: DMSO:75 mg/mL (209.22 mM);Ethanol:26 mg/mL (72.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.58 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC8:140 nM|HDAC10:40 nM|MBLAC2:<10 nM (EC50)|HDAC6:1008 nM|HDAC3:43 nM|HDAC11:93 nM|HDAC9:70 nM|HDAC5:47 nM|HDAC2:96 nM|HDAC7:137 nM|HDAC1:49 nM|HDAC4:56 nM
• In Vivo:
  SB939 exhibits selectivity for HDAC over non-HDAC enzymes, receptors, and ion channels that bind zinc by a factor of 100. It significantly inhibits Class II HDAC isoforms including HDAC4, HDAC5, HDAC7, HDAC9, and HDAC10, with IC50 values ranging from 40 nM to 137 nM, but does not affect HDAC6, as demonstrated by its IC50 of 1008 nM. Additionally, SB939 effectively inhibits Class IV enzyme HDAC11, with an IC50 of 93 nM, yet it lacks inhibitory activity against Class III HDACs, specifically SIRT1. Demonstrating significant antiproliferative activity against various tumor cell lines, especially leukemia cells and skin T-cell lymphoma cells, SB939's IC50 values range from 50 nM (in H9 cells) to 170 nM (in HEL92.1.7 cells).
• In Vitro:
  Administered at a dose of 50 mg/kg, SB939 selectively stimulates the growth of CT-116 xenograft tissues. It exhibits a tumor growth inhibition rate of 94% compared to SAHA. In nude mice, SB939 demonstrates superior pharmacokinetics and oral bioavailability than SAHA. Additionally, it inhibits adenoma formation in APC^min mice and enhances hematocrit levels more effectively than 5-fluorouracil. SB939 exhibits anticancer activity and high efficacy in various tumor models, including HCT-116, PC-3, A2780, MV4-11, and Ramos.
• Cell Research:
  Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.(Only for Reference)

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

SB 939, SB939, SB-939, Pracinostat, Histone deacetylases, HDAC8, HDAC9, HDAC1, HDAC, HDAC2, HDAC3, HDAC10, HDAC11, HDAC7, HDAC6, HDAC5, HDAC4, MBLAC2, inhibit, Inhibitor, cancer, Apoptosis

Compound Identifiers

PubChem CID

49855250