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 

Cat. No.: HY-12286 Purity: 98.78%
COA Handling Instructions

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

PI-1840 Chemical Structure

CAS No. : 1401223-22-0

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 83 In-stock
10 mg USD 130 In-stock
50 mg USD 468 In-stock
100 mg USD 864 In-stock
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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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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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Product Name:
PI-1840
Cat. No.:
HY-12286
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