DPP9-IN-2
DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection.
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- CAS No.: 3020859-44-0
- Formule: C33H33F2N3O2
- Masse moléculaire:541.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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DPP-9 12.9 nM (IC50) |
HIV-1 |
DPP9-IN-2 (Compound 6e) (0.05-5 μM; 24-48 h) induces pyroptosis in THP-1 cells, promoting LDH release and SYTOX Green uptake [1].
DPP9-IN-2 (0.5-5 μM; 24 h) induces pyroptosis depending on DPP9, CASP1, and GSDMD, and pyroptosis is significantly inhibited or delayed in DPP9-knockdown, CASP1-KO, or GSDMD-KO THP-1 cells[1].
DPP9-IN-2 (5 μM) shows weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitors (Efavirenz (HY-10572), Rilpivirine (HY-10574)) in MT-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | F | AUC0-last | Cl | Vd | T1/2 |
|---|---|---|---|---|---|---|---|---|
| Rat | 20 mg/kg | p.o. | 文献审核 | 61 % | 8176.1 ng·h/mL | / | / | / |
| Rat | 5 mg/kg | i.v. | 文献审核 | / | 3368.3 ng·h/mL | 1.5 L/h/kg | 23 L/kg | 10.9 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3020859-44-0
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Masse moléculaire 541.63
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Formule C33H33F2N3O2
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SMILES
O=C(C1=CC=C(C2=CC=C(F)C=C2)C=C1)NC34CC5(NCC(N6CC7=C(C=C(F)C=C7)C6)=O)CC(C4)CC(C5)C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DPP9-IN-2 Related Classifications
HY-179348 Related Classifications
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