1. Metabolic Enzyme/Protease Apoptosis Autophagy NF-κB Epigenetics Cell Cycle/DNA Damage
  2. Proteasome Apoptosis Autophagy Caspase Bcl-2 Family NF-κB PARP
  3. PI-1840

PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.

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PI-1840 Chemical Structure

PI-1840 Chemical Structure

CAS No. : 1401223-22-0

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Description

PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α[1][2].

In Vitro

PI-1840 (5-60 µM; 24 and 48 h) inhibits the proliferation of MG-63 and U2-OS cells[1].
PI-1840 (40 µM (U2-OS cells) and 60 µM (MG-63 cells); 24 and 48 h) induces cell cycle arrest at the G2/M phase[1].
PI-1840 (15-60 µM (MG-63 cells), 10-40 µM (U2-OS cells); 48 h) induces apoptosis through NF-κB pathway in MG-63 and U2-OS cells. PI-1840 induces autophagy in MG-63 and U2-OS cells[1].

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

Cell Viability Assay[1]

Cell Line: MG-63 and U2-OS cells
Concentration: 5, 10, 20, 40, 80, and 160 µM
Incubation Time: 24 and 48 hours
Result: Inhibited cell growth in a dose-dependent manner with IC50 values of 108.40 µM (MG-63, 24 h), 59.58 µM (MG-63, 48 h), 86.43 µM (U2-OS, 24 h), and 38.83 µM (U2-OS, 48 h), respectively.

Apoptosis Analysis[1]

Cell Line: MG-63 and U2-OS cells
Concentration: 15, 30, and 60 µM (MG-63 cells), 10, 20, and 40 µM (U2-OS cells)
Incubation Time: 48 hours
Result: Increased the apoptotic rates of the two cell lines in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MG-63 and U2-OS cells
Concentration: 40 µM (U2-OS cells) and 60 µM (MG-63 cells)
Incubation Time: 24 and 48 hours
Result: Increased in the G2/M phase cell population.

Western Blot Analysis[1]

Cell Line: MG-63 and U2-OS cells
Concentration: 40 µM (U2-OS cells) and 60 µM (MG-63 cells)
Incubation Time: 24 and 48 hours
Result: Increased the cell cycle regulation-associated proteins about p21, p27 and WEE1.

Western Blot Analysis[1]

Cell Line: MG-63 and U2-OS cells
Concentration: 15, 30, and 60 µM (MG-63 cells), 10, 20, and 40 µM (U2-OS cells)
Incubation Time: 48 hours
Result: Increased the ratio of the expression level of (p-IκBα/control)/(IκBα/control), and decreased the ratio of (p-p65/control)/(p65/control).
Decreased the expression level of Bcl-2 and the mitochondrial proteins Cyto c.
Increased the expression levels of Bax, and the ratios of (cleaved caspase-3/caspase-3, cleaved PARP/PARP, cleaved caspase-8/caspase-8 and cleaved caspase-9/caspase-9.
Increased the ratio of LC3 II to LC 3 I, and the expression level of Beclin1.
In Vivo

PI-1840 (150 mg/kg; i.p.; daily, for 14 d) inhibits the growth of human breast tumor xenografts in nude mice[2].

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

Animal Model: Female nude mice with MDA-MB-231 xenografts[2]
Dosage: 150 mg/kg
Administration: Intraperitoneal injection; daily, for 14 days
Result: Inhibited the growth of MDA-MB-231 tumor xenografts by 76%.
Molecular Weight

394.47

Formula

C22H26N4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C(C)C)CC1=NC(C2=CC=CN=C2)=NO1)COC3=CC=C(CCC)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (253.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5350 mL 12.6752 mL 25.3505 mL 63.3762 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL 12.6752 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL 6.3376 mL
15 mM 0.1690 mL 0.8450 mL 1.6900 mL 4.2251 mL
20 mM 0.1268 mL 0.6338 mL 1.2675 mL 3.1688 mL
25 mM 0.1014 mL 0.5070 mL 1.0140 mL 2.5350 mL
30 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1125 mL
40 mM 0.0634 mL 0.3169 mL 0.6338 mL 1.5844 mL
50 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2675 mL
60 mM 0.0423 mL 0.2113 mL 0.4225 mL 1.0563 mL
80 mM 0.0317 mL 0.1584 mL 0.3169 mL 0.7922 mL
100 mM 0.0254 mL 0.1268 mL 0.2535 mL 0.6338 mL
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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.

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PI-1840
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