2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. TPKI-39

TPKI-39 is a DDR1, DDR2, and FLT1 inhibitor, with a human DDR1 IC50 of 380 nM, human DDR1 Ka of 24 nM, human DDR2 IC50 of 120 nM, human FLT1 IC50 of 65 nM, and human FLT1 Ka of 91 nM.TPKI-39 inhibits DDR1 enzymatic activity and autophosphorylation, DDR2 enzymatic activity, and FLT1 enzymatic activity in cells.TPKI-39 inhibits collagen-induced DDR1 autophosphorylation in cells.

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TPKI-39

TPKI-39 Chemical Structure

CAS No. : 1005781-50-9

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TPKI-39 Related Antibodies

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Description

TPKI-39 is a DDR1, DDR2, and FLT1 inhibitor, with a human DDR1 IC50 of 380 nM, human DDR1 Ka of 24 nM, human DDR2 IC50 of 120 nM, human FLT1 IC50 of 65 nM, and human FLT1 Ka of 91 nM.TPKI-39 inhibits DDR1 enzymatic activity and autophosphorylation, DDR2 enzymatic activity, and FLT1 enzymatic activity in cells.TPKI-39 inhibits collagen-induced DDR1 autophosphorylation in cells[1].

In Vitro

TPKI-39 (1 μM; dose-response) potently engages DDR1, DDR2, and FLT1 in live HEK293 cells, with minimal to no engagement of most kinases identified as high-affinity binders in cell-free assays, and uniquely engages DDR2 in cells but not in cell-free systems[1].
TPKI-39 (0.313-5 μM; 1 h pretreatment, 24 h cotreatment with collagen I) potently inhibits DDR1 signaling (autophosphorylation) in HeLa cells stimulated with collagen I[1].

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

TPKI-39 Related Antibodies

Western Blot Analysis[1]

Cell Line: HeLa cells (transiently transfected with DDR1b-encoding cDNA)
Concentration: 0.313-5 μM (pretreated; cotreated with collagen I)
Incubation Time: 1 h (pretreatment); 24 h (cotreatment with collagen I)
Result: Dose-dependently inhibited collagen-induced DDR1 autophosphorylation.
Reduced phosphorylation to basal levels (observed without collagen activation) at concentrations ≥1.25 μM, comparable to the established DDR1 inhibitor DDR1-IN-1.
Molecular Weight

345.35

Formula

C19H15N5O2
CAS No.
SMILES

O=C(NC1=CC=CC(OC2=NN3C=CN=C3C=C2)=C1)NC4=CC=CC=C4
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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TPKI-39 Related Classifications

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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.

Keywords:

TPKI-391005781-50-9TPKI39TPKI 39Discoidin Domain ReceptorFLT1collagen Ienzymatic activitycollagenHeLa cellsautophosphorylationkinasesHEK293 cellsDDR2DDR1Inhibitorinhibitorinhibit

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