2. Anti-infection
  3. HBV
  4. DF-006

DF-006 is a first-in-class orally active agonist of ALPK1 (α-kinase 1). DF-006 can stimulate the innate immune response by activating the NF-κB pathway and strongly stimulate the innate immunity in the liver locally. DF-006 reduces the levels of serum HBV DNA (EC50 = 2.7 pM), HBsAg and HBeAg, and has shown strong antiviral effects. DF-006 is suitable for research on the immunotherapy of chronic hepatitis B (CHB).

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

DF-006 Chemical Structure

DF-006 Chemical Structure

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DF-006 Related Antibodies

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Description

DF-006 is a first-in-class orally active agonist of ALPK1 (α-kinase 1). DF-006 can stimulate the innate immune response by activating the NF-κB pathway and strongly stimulate the innate immunity in the liver locally. DF-006 reduces the levels of serum HBV DNA (EC50 = 2.7 pM), HBsAg and HBeAg, and has shown strong antiviral effects. DF-006 is suitable for research on the immunotherapy of chronic hepatitis B (CHB)[1].

In Vitro

DF-006 (0.3 pM-10 nM; 10-day treatment) potently suppresses HBV DNA (EC50 = 2.7 pM) in PHHs but failes to reduce cccDNA[1].
DF-006 selectively inhibits HBeAg secretion but not HBsAg in PHHs, suggesting differential modulation of viral antigen production [1].

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

DF-006 Related Antibodies

Real Time qPCR

Cell Line: Primary human hepatocytes (PHHs)
Concentration: 1 pM, 10 pM, 100 pM, 1 nM, 10 nM
Incubation Time: 72 h post-infection for 10 days
Result: Potently suppressed HBV DNA (EC50 = 2.7 pM)
Decreased encapsidated pgRNA (55%) and rcDNA (97%)
No significant reduction in cccDNA
Upregulated NF-κB target genes (TNF, IFN-β etc.)

ELISA Assay[1]

Cell Line: Primary human hepatocytes (PHHs)
Concentration: 1 pM, 10 pM, 100 pM, 1 nM, 10 nM
Incubation Time: 24 h post-infection for 10 days
Result: Reduced by up to 36% at 72 pM
No significant reduction observed
Parmacokinetics
Species Dose SampleTime Route
Mice 20 mg/kg 0, 2, 4, 8 hours post-dose p.o.
In Vivo

DF-006 (0.02-25 μg/kg; oral gavage; for 21-28 days) reduces serum HBV DNA (up to 2.4 log10), HBsAg (0.66 log10), and HBeAg, alongside decreases intrahepatic HBcAg (57%) and HBsAg [1].
DF-006 (10 μg/kg) combined with Entecavir (HY-13623) (ETV, 50 μg/kg) further reduces serum HBV DNA by 1.3 log10 versus monotherapy[1].

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

Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: 1 μg/kg, 5 μg/kg, 25 μg/kg
Administration: Oral gavage; once daily; for 28 days
Result: Reduced HBV DNA by 2.4 log10 copies/μL at 25 μg/kg.
Decreased HBsAg y 0.66 log10 IU/mL at 5 μg/kg and Significantly reduced at 5 μg/kg.
HBcAg nuclear staining decreased by 57% at 5 μg/kg.
Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: 0.02 μg/kg, 0.08 μg/kg, 0.25 μg/kg, 1 μg/kg
Administration: Oral gavage; once daily; for 21 days
Result: Potently suppressed HBV replication at doses as low as 0.08 μg/kg, with maximal efficacy at 25 μg/kg.
Reduced serum HBV DNA, HBsAg/HBeAg, and intrahepatic HBcAg/nucleocapsids.
No ALT elevation or overt toxicity, supporting clinical potential.
Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: DF-006 (10 μg/kg) combined with Entecavir (HY-13623) (ETV, 50 μg/kg)
Administration: Oral co-administration daily for 28 days
Result: Showed additive reduction of serum HBV DNA (1.3 log10 vs monotherapy).
Molecular Weight

791.54

Formula

C24H32FN5O18P2S
SMILES

NC1=NC=NC2=C1N=CN2[C@@H]3O[C@H](COP(OP(O[C@H]4[C@@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H]([C@H](OC(C)=O)F)O4)(O)=O)(O)=S)[C@@H](O)[C@H]3O
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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DF-006 Related Classifications

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× = ×
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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:

DF-006DF006DF 006HBVHepatitis B virusTIFA-TRAF6 signalingα-kinase 1chronic hepatitis BInhibitorinhibitorinhibit

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