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CAS No. 929016-96-6
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.
Selleck's Pracinostat (SB939) has been cited by 17 publications
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Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.
Antimicrob Agents Chemother 2012 56(7), 3849-56. Pracinostat (SB939) purchased from Selleck.
A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells.
Oncotarget, 2016, 7(23):34384-94. Pracinostat (SB939) purchased from Selleck.
(B) Immunoblots showing induction of apoptosis in K562 BIMi2+/+, BIMi2+/- and BIMi2-/-. The data shown are representative of 3 experiments with similar results. Cells were treated for 48hours with SB939 at the indicated concentrations. p-BCR-ABL, phosphorylated BCR-ABL; STAT5, signal transducer and activator of transcription 5; p-STAT5, phosphorylated STAT5; BIMEL, BIM extra long isoform; BIML, BIM long isoform; Cl. CASP3, cleaved CASPASE3; Cl. PARP, cleaved PARP. 48-hour treatment as in A.
PLoS One, 2017, 12(3):e0174107. Pracinostat (SB939) purchased from Selleck.
A: Mean fold change in γ-globin mRNA in erythroid progenitor cells treated with the designated therapeutic candidates (MS-275, SDMB, SB939, or Benserazide), compared to vehicle-treated cells from the same subject. All changes are significant, p <0.001. Error bars indicate SD. B. Mean change in proportions of cells expressing HbF protein (F-reticulocytes) in erythroid progenitor cells treated with therapeutic candidates (SDMB, Benserazide, MS275, SB939), compared to control cells from the same subject. Error bars indicate SD. * Asterisks indicate statistically significant differences (* p<0.05, ** p<0.01. *** p<0.001)
Blood Cells Mol Dis, 2016, 56(1):62-9. Pracinostat (SB939) purchased from Selleck.
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|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.|
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). 
|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 than 5-fluorouracil. |
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.
|In vitro||DMSO||72 mg/mL (200.84 mM)|
|Ethanol||27 mg/mL (75.31 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02118909||Completed||Drug: Pracinostat|Drug: Itraconazole|Drug: Ciprofloxacin||Healthy Volunteers|Non-smokers||Helsinn Healthcare SA||May 2014||Phase 1|
|NCT02058784||Completed||Drug: pracinostat||Healthy Volunteers|Moderate to Heavy Smokers|Non-smokers||Helsinn Healthcare SA|Celerion||February 2014||Early Phase 1|
|NCT01112384||Completed||Drug: SB939||Metastatic Sarcoma||NCIC Clinical Trials Group|S*BIO|Canadian Cancer Trials Group||March 18 2010||Phase 2|
|NCT00741234||Completed||Drug: SB939|Drug: Azacitidine||Solid Tumors|Hematologic Malignancies|Myelodysplastic Syndrome||S*BIO||April 2007||Phase 1|
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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