Cat. No.: HY-12286

PI-1840

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Based on 1 Customer Validation

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.

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

Purity: 98.78%
CAS No.: 1401223-22-0
Formula: C₂₂H₂₆N₄O₃
Molecular Weight:394.47

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PI-1840 Chemical Structure

CAS No.: 1401223-22-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

All NF-κB Isoforms :

All PARP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	2.95 nM Compound: 6; PI-1840	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30391816]
HGC-27	IC₅₀	3.35 nM Compound: 6; PI-1840	Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 72 hrs by MTT assay	[PMID: 30391816]
MDA-MB-231	IC₅₀	7.6 μM Compound: PI-1840	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay	[PMID: 32853683]
MM1.S	IC₅₀	>20 nM Compound: 6; PI-1840	Antiproliferative activity against human MM1S cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human MM1S cells after 72 hrs by MTS/PMS assay	[PMID: 30391816]
MV4-11	IC₅₀	>20 nM Compound: 6; PI-1840	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS/PMS assay	[PMID: 30391816]
RPMI-8226	IC₅₀	>20 nM Compound: 6; PI-1840	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS/PMS assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS/PMS assay	[PMID: 30391816]

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%.

Chemical Information

CAS No. 1401223-22-0
Appearance Solid
Molecular Weight 394.47
Formula C₂₂H₂₆N₄O₃
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5350 mL

12.6752 mL

25.3505 mL

5 mM

0.5070 mL

2.5350 mL

5.0701 mL

10 mM

0.2535 mL

1.2675 mL

2.5350 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kazi A, et, al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Apr 25;289(17):11906-11915. [Content Brief]

[2]. Chen Y, et, al. Non covalent proteasome inhibitor PI 1840 induces apoptosis and autophagy in osteosarcoma cells. Oncol Rep. 2019 May;41(5):2803-2817. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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PI-1840

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Pyroptosis Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

MCE Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All Caspase Isoforms

All Bcl-2 Family Isoforms

All NF-κB Isoforms

All PARP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PI-1840 Related Classifications

HY-12286 Related Classifications