Home Cytoskeletal Signaling HDAC inhibitor - Apoptosis related activator Pracinostat (SB939) For research use only.

Pracinostat (SB939)

Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.

Pracinostat (SB939) Chemical Structure

Pracinostat (SB939) Chemical Structure

CAS No. 929016-96-6

Purity & Quality Control

Pracinostat (SB939) Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.17 μM 24119555
NCI-H460 cells Proliferation assay 48 h Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.22 μM 24119555
HCT116 cells Proliferation assay 48 h Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.24 μM 24119555
MDA-MB-435 cells Proliferation assay 48 h Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.48 μM 24119555
OVCAR5 cells Proliferation assay 48 h Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=0.61 μM 24119555
HepG2 Antimalarial assay Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells, IC50 = 0.15 μM. 24904967
HepG2 Antiplasmodial assay 53 hrs Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method, IC50 = 0.15 μM. 28241112
Sf9 Function assay 2 hrs Inhibition of recombinant human HDAC-2 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM. ChEMBL
HEK293-F Function assay 2 hrs Inhibition of recombinant human HDAC-8 expressed in HEK293-F cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM. ChEMBL
Sf9 Function assay 2 hrs Inhibition of recombinant human HDAC-1 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM. ChEMBL
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Biological Activity

Description Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.
Features A new histone deacetylase inhibitor based on hydroxamic acid, with improved physicochemical, pharmaceutical, and pharmacokinetic properties.
Targets
HDAC10 [1]
(Cell-free assay)		 HDAC3 [1]
(Cell-free assay)		 HDAC5 [1]
(Cell-free assay)		 HDAC1 [1]
(Cell-free assay)		 HDAC4 [1]
(Cell-free assay)		 Click to View More Targets
40 nM 43 nM 47 nM 49 nM 56 nM
In vitro
In vitro

SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. SB939 is a potent inhibitor of HDAC class I isoenzymes, HDAC1, HDAC2, HDAC3 and HDAC8 with the IC50 values ranging from 43 nM to 140 nM. SB939 inhibits HDAC class II isoenzymes , HDAC4, HDAC5, HDAC7, HDAC9 and HDAC10 significantly with the IC50 values ranging from 40 nM to 137 nM, with the exception of HDAC6 which shows IC50 of 1008 nM. It markedly inhibits HDAC11 of the HDAC class IV enzymes with IC50 of 93 nM, but shows no inhibitory activity against SIRT 1 of the class III HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, especially Leukemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells). [1]
Kinase Assay HDAC enzyme assay
All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software.
Cell Research Cell lines HCT116, A2780, ACHN, MCF7, HL-60, et al.
Concentrations Dissolved in DMSO (stock concentration, 10 mM), final concentrations 1.5 nM to 100 μM
Incubation Time 96 hours
Method

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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-JAK2 / JAK2 / p-STAT5 / STAT5 / p-FLT3 / FLT3 22829971
In Vivo
In vivo

Administration of SB939 (25 mg/kg to 100 mg/kg) displays a dose-dependent antitumor efficacy in a xenograft mice model of human colorectal cancer (HCT-116). This is approximately twice as efficacious as SAHA: SB939 causing a tumor growth inhibition of 94% versus 48% by SAHA with both at the maximum tolerated dose. Oral administration of SB939 at a dose of 50 mg/kg or 75 mg/kg in the APCmin genetic mice model of early-stage colon cancer markedly reduces the number of tumors , decreases cumulative hemocult scores and increases hematocrit values more effectively. [1]
Animal Research Animal Models BALB/c nude mice bearing HCT-116 human colon cancer xenografts, Male and APCmin mice
Dosages 25, 50, 75, or 100 mg/kg
Administration Oral gavage once daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02118909 Completed
Healthy Volunteers|Non-smokers
Helsinn Healthcare SA
 May 2014 Phase 1
NCT02058784 Completed
Healthy Volunteers|Moderate to Heavy Smokers|Non-smokers
Helsinn Healthcare SA|Celerion
 February 2014 Early Phase 1
NCT01112384 Completed
Metastatic Sarcoma
NCIC Clinical Trials Group|S*BIO|Canadian Cancer Trials Group
 October 21 2010 Phase 2
NCT00741234 Completed
Solid Tumors|Hematologic Malignancies|Myelodysplastic Syndrome
S*BIO
 April 2007 Phase 1

Chemical Information & Solubility

Molecular Weight 358.48 Formula

C20H30N4O2
CAS No. 929016-96-6 SDF Download Pracinostat (SB939) SDF
Smiles CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=O)NO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (200.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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