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Chemical Structure| 1401223-22-0 Chemical Structure| 1401223-22-0

Structure of PI-1840
CAS No.: 1401223-22-0

Chemical Structure| 1401223-22-0

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PI-1840 is an effective selective cathepsin L (CT-L) inhibitor with an IC50 of 27 nM. PI-1840 inhibits cell proliferation, arrests the cell cycle at the G2/M phase, induces apoptosis, and autophagy.

Synonyms: PI-1840

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Product Details of PI-1840

CAS No. :1401223-22-0
Formula : C22H26N4O3
M.W : 394.47
SMILES Code : O=C(N(C(C)C)CC1=NC(C2=CC=CN=C2)=NO1)COC3=CC=C(CCC)C=C3
Synonyms :
PI-1840
MDL No. :MFCD28142700

Safety of PI-1840

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PI-1840

epigenetics
DNA
pyroptosis

Isoform Comparison

Biological Activity

Target
  • 20S proteasome

    Chymotrypsin-like proteasome, IC50:27 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-468 human breast cancer cells 0.37 μM 2 hours Inhibited CT-L activity PMC3774303
U2-OS 0, 20, 40 µM 48 hours To evaluate the inhibitory effect of PI-1840 on the proliferation of U2-OS cells, results showed that PI-1840 inhibited cell proliferation in a dose-dependent manner and altered cell morphology. PMC6448088
MG-63 0, 30, 60 µM 48 hours To evaluate the inhibitory effect of PI-1840 on the proliferation of MG-63 cells, results showed that PI-1840 inhibited cell proliferation in a dose-dependent manner and altered cell morphology. PMC6448088
MCF-10A 20 μM 2 hours To evaluate the inhibitory effect of PI-1840 on CT-L activity, results showed that PI-1840 inhibited CT-L activity by 63.2 ± 5.4% at 20 μM. PMC4002098
LNCaP 20 μM 2 hours To evaluate the inhibitory effect of PI-1840 on CT-L activity, results showed that PI-1840 inhibited CT-L activity by 88.8 ± 1.0% at 20 μM. PMC4002098
HCT-116 20 μM 2 hours To evaluate the inhibitory effect of PI-1840 on CT-L activity, results showed that PI-1840 inhibited CT-L activity by 88.4 ± 4.6% at 20 μM. PMC4002098
MDA-MB-468 20 μM 2 hours To evaluate the inhibitory effect of PI-1840 on CT-L activity, results showed that PI-1840 inhibited CT-L activity by 63.2 ± 5.4% at 20 μM. PMC4002098
AsPC-1 cells 100 μM PI-1840 or 50 μg/ml trypsin inhibitor 72 hours To assess the effect of PI-1840 and trypsin inhibitor on cell viability. Only the chymotrypsin inhibitor blocked cell death. PMC8924000

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Human breast cancer MDA-MB-231 xenograft model Intraperitoneal injection 150 mg/kg Daily for 14 days To evaluate the anti-tumor effect of PI-1840 on human breast cancer MDA-MB-231 xenograft model, results showed that PI-1840 significantly inhibited tumor growth with an inhibition rate of 76%. PMC4002098

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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