GLPBio

Pracinostat (SB939)

Catalog No.: GC16734Purity:>99.50%Synonyms: Pracinostat

A pan-HDAC inhibitor

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Pracinostat (SB939)
Cas No.: 929016-96-6
10mM (in 1mL DMSO)In Stock
$100.00
1
5mgIn Stock
$79.00
1
10mgIn Stock
$151.00
1
50mgIn Stock
$432.00
1

Citations

Aucune citation n’est actuellement disponible pour ce produit. Vous trouverez ci-dessous une sélection de publications citant des produits GlpBio.
  • Nature cover
    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    Science
    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    Cell Research
    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

Description

Pracinostat, also known as SB939, is a potent and orally available inhibitor of histone deacetylase (HDAC) with a relatively stronger selectivity (more than 1000-fold) for class I, class II and class IV HDACs rather than class III HDACs. Pracinostat potently suppresses proliferation in a wide range of cancer cell lines, including colon cancer, ovarian cancer, prostate carcinomas, acute myeloid leukaemia (AML) and B cell lymphoma. Recent study results have shown that SB939 induces the accumulation of acetylated histone H3 (AcH3) and acetylated α-tubulin and increases the expression of the cyclin dependent kinase inhibitor p21 in cancer cells.

Reference

[1].Razak AR, Hotte SJ, Siu LL, Chen EX, Hirte HW, Powers J, Walsh W, Stayner LA, Laughlin A, Novotny-Diermayr V, Zhu J, Eisenhauer EA. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br J Cancer. 2011;104(5):756-762.

Protocole (Protocol)

Cell experiment:

Cell lines

Ovarian (A2780) , colon (HCT-116), and prostate (PC-3) cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

96 h; IC50=0.48±0.21 μM (A2780), 0.48±0.27 μM (HCT-116), 0.34±0.06 μM (PC-3)

Applications

SB939 showed broad anti-proliferative activity against representative tumor cells from ovarian (A2780) , colon (HCT-116), and prostate (PC-3) with cellular IC50 values of 0.48±0.21, 0.48±0.27 and 0.34±0.06 μM, respectively.

Animal experiment:

Animal models

Athymic nude mice

Dosage form

200 mg/kg, 100 mg/kg, 50 mg/kg; oral taken.

Applications

SB939 was clearly toxic at the highest dose tested (200 mg/kg); however, at the MTD dose of 100 mg/kg and at 50mg/kg, it demonstrated very significant antitumor effects on day 21 with TGI = 90% (p < 0.001 ) and 66% ( p < 0.001), respectively, with acceptable body weight loss.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang H, Yu N, Chen D, et al. Discovery of (2 E)-3-{2-butyl-1-[2-(diethylamino) ethyl]-1 H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile[J]. Journal of medicinal chemistry, 2011, 54(13): 4694-4720.

Documents produit (Product Documents)

Purity:>99.50%Appearance:A solid

Propriétés chimiques (Chemical Properties)

N° CAS
929016-96-6
Synonymes
Pracinostat
Nom chimique
(E)-3-[2-butyl-1-[2-(diethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide
SMILES
CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=O)NO
Formule moléculaire
C20H30N4O2
Masse moléculaire
358.48
Solubilité
≥ 11.4 mg/mL in DMSO, ≥ 24.8 mg/mL in EtOH with ultrasonic
Conservation
Store at -20°C
Conseils généraux
Choisissez un solvant adapté selon les données de solubilité du produit. Après préparation, répartissez la solution mère en aliquotes afin d’éviter les cycles répétés de congélation-décongélation.
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Conditions d’expédition
Les échantillons d’évaluation sont expédiés avec des blocs réfrigérants. Les autres formats sont expédiés à température ambiante ou, sur demande, avec des blocs réfrigérants.

Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité

g/mol

Reviews

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