2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Enpp-1-IN-30

Enpp-1-IN-30 (compound 44a) is an orally active ENPP1 inhibitor with a human IC50 of 13.1 nM. Enpp-1-IN-30 prevents cGAMP degradation, activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance innate immune response. Enpp-1-IN-30 exerts antitumor efficacy in syngeneic mouse models. Enpp-1-IN-30 can be used for the research of colon carcinoma.

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

Enpp-1-IN-30

Enpp-1-IN-30 Chemical Structure

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Enpp-1-IN-30 Related Antibodies

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Description

Enpp-1-IN-30 (compound 44a) is an orally active ENPP1 inhibitor with a human IC50 of 13.1 nM. Enpp-1-IN-30 prevents cGAMP degradation, activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance innate immune response. Enpp-1-IN-30 exerts antitumor efficacy in syngeneic mouse models. Enpp-1-IN-30 can be used for the research of colon carcinoma[1].

In Vitro

Enpp-1-IN-30 (compound 44a) (0.2 nM-1 μM; 2 h) potently inhibits recombinant human ENPP1 with an IC50 of 13.1 nM[1].
Enpp-1-IN-30 (up to 10,000 nM) is highly selective for ENPP1, with no detectable inhibition of recombinant human ENPP2 or ENPP3 at concentrations up to 10,000 nM[1].
Enpp-1-IN-30 (0.01-30 μM; 1 h) dose-dependently enhances cGAMP-mediated STING pathway activation in HCT116-Dual? cells, achieving an 8.8-fold increase in IRF3 luciferase intensity at 10 μM and a 10.1-fold increase at 30 μM[1].
Enpp-1-IN-30 (10 μM; 1-72 h) enhances innate immune activation in THP-1 cells co-treated with cGAMP, significantly increasing IFNB and CXCL10 mRNA expression over time and inducing a gradual, non-excessive increase in TNFA mRNA expression[1].

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

Enpp-1-IN-30 Related Antibodies

Real Time qPCR[1]

Cell Line: THP-1 cells
Concentration: 10 μM (co-treated with 10 μM cGAMP)
Incubation Time: 24-72 h (IFNB); 1-72 h (CXCL10, TNFA)
Result: Increased IFNB mRNA expression by 6.7-fold at 72 h (co-treated with 10 μM cGAMP).
Increased CXCL10 mRNA expression by 137-fold at 72 h (co-treated with 10 μM cGAMP).
Induced a gradual increase in TNFA mRNA expression reaching 8-fold at 72 h (co-treated with 10 μM cGAMP), with no instant overexpression of TNFA.
Parmacokinetics
Species Dose Route AUClast Cmax Tmax T1/2 Bioavailability CL Vss
Mice[1] 2 mg/kg i.v. 6949 ng·h/mL 3613 ng/mL / 2.42 h / 284 mL/min/kg 658 L/kg
Mice[1] 10 mg/kg p.o. 23464 ng·h/mL 4526 ng/mL 0.5 h 2.97 h 65.8 % / /
In Vivo

Enpp-1-IN-30 (compound 44a) (50 mg/kg; p.o.; once daily; 14 days) significantly reduces tumor volume in the MC38 syngeneic colon carcinoma mouse model, with synergistic efficacy observed in combination with anti-mPD-L1 antibody, and no associated toxicity[1].

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

Animal Model: C57BL/6 (7-week-old female)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily; 14 days
Result: Reduced tumor volumes significantly relative to vehicle control group.
Produced synergistic tumor volume reduction in combination with anti-mPD-L1 antibody.
Caused no significant body weight loss or other clinical signs of toxicity.
Molecular Weight

349.38

Formula

C15H16FN5O2S
SMILES

C[S@](=O)(NCC1=CC=C(N2N=NC3=CC(OC)=CC=C32)C(F)=C1)=N
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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Enpp-1-IN-30 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:

Enpp-1-IN-30Phosphodiesterase (PDE)THP-1 cellscGAMPinnate immune responseSTING pathwaysyngeneic mouse modelsENPP2colon carcinomaENPP3ENPP1HCT116-Dual? cellsInhibitorinhibitorinhibit

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