2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. DDR1/2 IN-4

DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis.

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

DDR1/2 IN-4

DDR1/2 IN-4 Chemical Structure

CAS No. : 3027967-95-6

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.

DDR1/2 IN-4 Related Antibodies

Top Publications Citing Use of Products

View All Discoidin Domain Receptor Isoform Specific Products:

View All Isoforms
DDR1 DDR2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis[1].

IC50 & Target[1]

DDR1

8.6 (pKi)

DDR2

8.2 (pKi)

In Vitro

DDR1/2 IN-4 potently binds to DDR1 (pKi=8.6) and DDR2 (pKi=8.2)[1].
DDR1/2 IN-4 potently inhibits DDR1 activity in U2OS cells, with a pIC50 of 8.0[1].
DDR1/2 IN-4 (1-30 μM; 48 h) shows no cytotoxicity against A549 cells at concentrations up to 10 μM, and only exhibits mild cytotoxicity after 48 h treatment at 30 μM[1].

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

DDR1/2 IN-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: A549 cells
Concentration: 1-30 μM
Incubation Time: 48 h
Result: Showed no cytotoxicity at concentrations up to 10 μM; reduced cell viability to 84.9% at 30 μM.
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) T1/2 AUClast
Mice[1] 1 mg/kg i.n. 117 (plasma) ng/g 0.083 (plasma) h 2 (plasma) h 141 (plasma) ng·h/mL
In Vivo

DDR1/2 IN-4 (0.1-1 mg/kg; intranasal; single administration) significantly reduces collagen-induced pulmonary MCP-1 levels by 39% in male C57BL/6N mice, confirming its in vivo activity of inhibiting DDR-mediated signaling pathways[1].

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

Animal Model: C57BL/6N (male)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Administration: intranasal; single dose
Result: Showed dose-dependent inhibition of pulmonary MCP-1 levels.
Caused a significant 39% reduction in pulmonary MCP-1 levels compared to the vehicle-treated, collagen-challenged group (p < 0.05) at 1 mg/kg.
Molecular Weight

467.45

Formula

C23H20F3N7O
CAS No.
SMILES

O=C(NC1=CC(C(F)(F)F)=CN=C1)C2=CC=C(C)C(NC3CN(C4=C5C=NC=CN5N=C4)C3)=C2
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.

DDR1/2 IN-4 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:

DDR1/2 IN-43027967-95-6Discoidin Domain ReceptorABL1 kinaseDDR1idiopathic pulmonary fibrosishERG-HEK cellsC57BL/6N miceDDR2A549 cellscollagen-induced mouse modelmiceU2OS cellsInhibitorinhibitorinhibit

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:
DDR1/2 IN-4
Cat. No.:
HY-181839
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.