2. Anti-infection Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Beta-lactamase HDAC Apoptosis
  4. Pracinostat

Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM.

For research use only. We do not sell to patients.

Pracinostat Chemical Structure

Pracinostat Chemical Structure

CAS No. : 929016-96-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 140 In-stock
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Solid
1 mg USD 51 In-stock
5 mg USD 127 In-stock
10 mg USD 220 In-stock
50 mg USD 780 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Pracinostat:

Pracinostat Related Antibodies

Top Publications Citing Use of Products

View All Beta-lactamase Isoform Specific Products:

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Metallo-β-lactamase

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View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM[1][4].

IC50 & Target[1][4]

HDAC10

40 nM (IC50)

HDAC3

43 nM (IC50)

HDAC5

47 nM (IC50)

HDAC1

49 nM (IC50)

HDAC4

56 nM (IC50)

HDAC9

70 nM (IC50)

HDAC11

93 nM (IC50)

HDAC2

96 nM (IC50)

HDAC7

137 nM (IC50)

HDAC8

140 nM (IC50)

HDAC6

1008 nM (IC50)

MBLAC2

<10 nM (EC50)

In Vitro

Pracinostat (SB939) is a potent novel hydroxamate-based inhibitor of HDACs class I, II, and IV, inhibiting the isolated enzymes with a Ki of 19 to 48 nM (class I), 16 to 247 nM (class II), and 43 nM (class IV), but with no activity against the class III isoenzyme SIRT I. SB939 has effects on HCT-116 colon cancer cell line and the HL-60 acute myeloid leukemia cell line, with IC50s of 0.48 μM and 70 nM, respectively. SB939 does not inhibit the proliferation of normal human dermal fibroblasts at concentrations up to 100 μM[1]. Pracinostat (SB939, compound 3) inhibits CYP2C19 with IC50 of 5.78 μM. SB939 shows potent activities against A2780, COLO 205, HCT-116, and PC-3 cell lines, with IC50s of 0.48 ± 0.21, 0.56 ± 0.08, 0.48 ± 0.27, and 0.34 ± 0.06[2]. Pracinostat downregulates JAK and FLT3 signaling in JAK2V617F and FLT-ITD cell lines, and shows synergy in combination with pacritinib. Pracinostat and pacritinib show in vitro synergy on STAT signaling and apoptosis. Pracinostat potently inhibits proliferation of different AML subtypes as a single agent and is synergistic with pacritinib in JAK2V617F or FLT3-ITD AML cell lines[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pracinostat Related Antibodies
In Vivo

Pracinostat (SB939, 25-100 mg/kg) shows significant dose-dependent growth inhibition of HCT-116 xenografts. SB939 selectively accumulates in tumor tissue. SB939 (50 or 75 mg/kg) exhibits anti-tumor activities in the Apcmin genetic colon cancer mouse model[1]. Pracinostat (25 or 50 mg/kg per day for 21 days) induces significant inhibition of tumor growth (TGI), by 59 and 116%, respectively, in mice bearing MV4-11 xenografts. Pracinostat (75 mg/kg, q.o.d) in combination with pacritinib is efficacious and synergistic in vivo in two different models of human AML. Pracinostat and pacritinib have synergistic effects on AML-induced plasma cytokines/growth factors/chemokines[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

358.48

Formula

C20H30N4O2
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

ONC(/C=C/C1=CC=C2N(C(CCCC)=NC2=C1)CCN(CC)CC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (697.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7896 mL 13.9478 mL 27.8956 mL
5 mM 0.5579 mL 2.7896 mL 5.5791 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (7.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.82%

COA (246 KB) HNMR (276 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Cells are seeded in 96-well plates at a predetermined optimal density, in the log growth phase, and rested for 24 h (adherent cells) or 2 h (suspension cells), respectively, before treatment with SB939. All experiments are done in triplicates for 96 h, with 1% solvent, using either the CyQUANT Cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells, in a total volume of 100 μL with SB939 concentrations from 100 μM to 1.5 nM in nine serial dilution steps. IC50 are determined using the XLfit software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Male ApcMin/+ mice and female C57BL/6 mice are fed a standard rodent diet. Mice with the confirmed mutation, between 16 and 20.5 wk of age, with a positive scoring in the hemocult assay are recruited to the experiment. During treatment, mice are injected i.p. with 40 mg/kg of 5-FU in a volume of 200 μL per 20 g body weight, once daily, for 5 d of treatment, followed by a 9-d recovery period and an additional 5 d of treatment. Treatment with SB939 per oral at 50 or 75 mg/kg once daily is given continuously for 21 d. At the last day of the treatment, the small intestine, caecum, and colon are removed; fixed by multiple injections of 4% PBS-buffered formaldehyde into the gut lumen; cut into segments; and spread flat on a plastic film in a formaldehyde bath. Tumor load is measured in a dissection microscope. Assessment and analysis of the samples are done blinded[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7896 mL 13.9478 mL 27.8956 mL 69.7389 mL
5 mM 0.5579 mL 2.7896 mL 5.5791 mL 13.9478 mL
10 mM 0.2790 mL 1.3948 mL 2.7896 mL 6.9739 mL
15 mM 0.1860 mL 0.9299 mL 1.8597 mL 4.6493 mL
20 mM 0.1395 mL 0.6974 mL 1.3948 mL 3.4869 mL
25 mM 0.1116 mL 0.5579 mL 1.1158 mL 2.7896 mL
30 mM 0.0930 mL 0.4649 mL 0.9299 mL 2.3246 mL
40 mM 0.0697 mL 0.3487 mL 0.6974 mL 1.7435 mL
50 mM 0.0558 mL 0.2790 mL 0.5579 mL 1.3948 mL
60 mM 0.0465 mL 0.2325 mL 0.4649 mL 1.1623 mL
80 mM 0.0349 mL 0.1743 mL 0.3487 mL 0.8717 mL
100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6974 mL
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Pracinostat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pracinostat929016-96-6SB939SB 939SB-939Beta-lactamaseHDACApoptosisβ-lactamaseHistone deacetylasescancerMBLAC2Inhibitorinhibitorinhibit

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