2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. PI3K-001

PI3K-001 is a cathepsin B-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsin B-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis.

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

PI3K-001

PI3K-001 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

PI3K-001 Related Antibodies

Top Publications Citing Use of Products

View All Cathepsin Isoform Specific Products:

View All Isoforms
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PI3K-001 is a cathepsin B-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsin B-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis[1].

In Vitro

PI3K-001 (50 μM; 30 min at 37 °C) binds to albumin with a rate exceeding 97% in both human and mouse plasma[1].
PI3K-001 (50 μM; 1-7 days at 37 °C) exhibits high plasma stability, with less than 1% release of its active payload P001 over 7 days of incubation at 37 °C in both human and mouse plasma[1].

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

PI3K-001 Related Antibodies
In Vivo

PI3K-001 (9.5 mg/kg; i.v.; single dose) achieves targeted delivery of P001 to fibrotic lung tissue and sustains drug presence in lung tissue for at least 18 h[1].
PI3K-001 (25 mg/kg; i.v.; once every 7 days; 2 total doses) exhibits superior antifibrotic efficacy in a bleomycin-induced pulmonary fibrosis mouse model, including significantly improved survival, reduced body weight loss, and reduced lung fibrosis markers compared to the parent drug P001[1].
PI3K-001 (3 mg/kg; i.v.; single dose) demonstrates improved pharmacokinetic properties in healthy SD rats, with 10-fold higher Cmax and 7-fold higher AUC than the parent drug P001, indicating enhanced systemic exposure and prolonged circulation[1].

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

Animal Model: C57BL/6 (male, 20-22 g, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 9.5 mg/kg
Administration: i.v.; single dose
Result: Delivered P001 to lung tissue at a concentration significantly higher than the parent P001 group at 6 h post-administration.
Maintained detectable P001 in lung tissue at up to ~50 ng/g at 18 h post-administration, while P001 was nearly undetectable in lung tissue.
Animal Model: C57BL/6 (male, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 25 mg/kg
Administration: i.v.; once every 7 days; 2 total doses
Result: Significantly improved mouse survival compared to the P001 group.
Reduced body weight loss relative to the P001 group.
Produced statistically significant reductions in bleomycin-induced increases in lung weight and lung index, with greater improvement than P001 and the positive control nintedanib.
Significantly reduced lung collagen deposition and preserved alveolar structure, with lung tissue morphology closer to normal than the P001 group, as shown by Masson and H&E staining.
Molecular Weight

1704.95

Formula

C82H111F2N11O22S2
SMILES

COC1=C(C=C(C=N1)C2=CC3=C(N=CC=C3C4=CN=C(C=C4)COCN(C(OCC5=CC=C(C=C5)NC([C@@H](NC([C@H](C(C)C)NC(COCCOCCNC(COCCOCCNC(CC[C@@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)C)=O)=O)CCS(C)(=O)=O)C=C2)NS(=O)(C6=CC=C(C=C6F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PI3K-001 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

PI3K-001CathepsinEPR effectalbuminalveolar damagemouse plasmacollagen depositionpulmonary fibrosisbleomycin-induced pulmonary fibrosis mouse modelcathepsin Bhuman plasmafibrotic lung lesionsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PI3K-001
Cat. No.:
HY-181741
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.