PI-1840

Cat. No.: HY-12286 Purity: 98.78%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

PI-1840 Chemical Structure

CAS No. : 1401223-22-0

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 192	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 298	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 447	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Caspase Isoform Specific Products:

View All Isoforms

Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

View All NF-κB Isoform Specific Products:

View All Isoforms

NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All PARP Isoform Specific Products:

View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
Customer Review

Description

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%.

Molecular Weight

394.47

Formula

C₂₂H₂₆N₄O₃

CAS No.

1401223-22-0

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
10 mM	0.2535 mL	1.2675 mL	2.5350 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:

Dosage

mg/kg

Animal weight
(per animal)

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: 98.78%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (245 KB) LCMS (87 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]

Complete Stock Solution Preparation Table

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

PI-1840 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.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

PI-1840

PI-1840 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Caspase Isoform Specific Products:

View All Bcl-2 Family Isoform Specific Products:

View All NF-κB Isoform Specific Products:

View All PARP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PI-1840 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PI-1840 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report