1. Metabolic Enzyme/Protease Anti-infection Immunology/Inflammation Apoptosis
  2. Dipeptidyl Peptidase HIV Pyroptosis
  3. 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.

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

DPP9-IN-2

DPP9-IN-2 Chemical Structure

CAS No. : 3020859-44-0

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Description

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[1].

IC50 & Target[1]

DPP-9

12.9 nM (IC50)

HIV-1

 

In Vitro

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.

Parmacokinetics
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
In Vivo

DPP9-IN-2 (Compound 6e) (5 mg/kg for i.v. or 20 mg/kg for p.o. ) increases the necrosis rate of CD3⁻CD11b⁻ leukocytes (such as B cells and NK cells) in Wistar rats[1].

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

Molecular Weight

541.63

Formula

C33H33F2N3O2

CAS No.
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

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
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  • 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.

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Product Name:
DPP9-IN-2
Cat. No.:
HY-179348
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